| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| PF 3654746 - PF 03654746 | Axon 1458
CAS [1039399-17-1]
MF C18H24F2N2O.C7H8O3SMW 494.59
Purity:
99%
Soluble in water and DMSO
Description
Histamine H3 receptor antagonist; investigational therapeutic for attention-deficit hyperactivity disorder (ADHD).
KEYWORDS: PF 3654746 | supplier | H3 antagonist | PF 03654746 | PF3654746 | PF03654746 | PF-3654746 | PF-03654746 | CAS [1039399-17-1] | [935840-31-6] | Histamine | GPCR | investigational therapeutic | ADHD | attention-deficit hyperactivity disorder | | axonmedchem |
| Fexofenadine hydrochloride | Axon 1453
CAS [153439-40-8]
MF C32H39NO4.HClMW 538.12
Purity:
99%
Soluble in DMSO
Description
Histamine H1 receptor antagonist; antihistamine drug in the treatment of hayfever and similar allergy symptons
References
Certificates
Categories
Extra info
PV Dicpinigaitis and YE Gayle. Effect of the second-generation antihistamine, fexofenadine, on cough reflex sensitivity and pulmonary function. Br. J. Clin. Pharmacol. 2003, 56 (5), 501–504.
GA Vena et al. Fexofenadine in chronic idiopathic urticaria: a clinical and immunohistochemical evaluation. Int. J. Immunopathol. Pharmacol. 2002, 15 (3), 217–224.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Pain & Inflammation
H1
A18
H1 antagonist
Chemical name
2-(4-{1-Hydroxy-4-[4-(hydroxy-diphenyl-methyl)-piperidin-1-yl]-butyl}-phenyl)-2-methyl-propionic acid
Parent CAS No.
[83799-24-0]
Order
Size
Unit Price
Stock
10 mg
€55.00
In Stock | | axonmedchem |
| Iodophenpropit dihydrobromide | Axon 1328
CAS [145196-87-8]
MF C15H19IN4S.2HBrMW 576.13
Purity:
98%
Soluble in DMSO and Ethanol
Description
Potent and selective histamine H3 receptor antagonist.
KEYWORDS: Iodophenpropit dihydrobromide | supplier | H3 antagonist | Iodophenpropit | VUF4586 | VUF-4586 | CAS [145196-87-8] | CAS [145196-88-9] | Histamine | H3 | Antagonist | Receptors | | axonmedchem |
| Immethridine dihydrobromide | Axon 1327
CAS [699020-93-4]
MF C9H9N3.2HBrMW 321.01
Purity:
98%
Soluble in water and DMSO
Description
Potent and selective histamine H3 receptor agonist.
KEYWORDS: Immethridine dihydrobromide | supplier | H3 agonist | CAS [699020-93-4] | [87976-03-2] | Axon Medchem | Axon 1327 | Histamine | H3 | Agonist | Receptors | | axonmedchem |
| Immepip dihydrobromide | Axon 1326
CAS [164391-47-3]
MF C9H15N3.2HBrMW 327.06
Purity:
98%
Soluble in water and DMSO
Description
Potent histamine H3 receptor agonist; also with affinity at histamine H4 receptor.
KEYWORDS: Immepip HBr | supplier | H3/H4 agonist | CAS [164391-47-3] | [151070-83-6] | Histamine | H3 | H4 | GPCR | CNS | sleep-wake cycle | | axonmedchem |
| Imetit dihydrobromide | Axon 1325
CAS [32385-58-3]
MF C6H10N4S.2HBrMW 332.06
Purity:
98%
Soluble in water
Description
Potent and specific histamine H3 receptor agonist
References
Certificates
Categories
Extra info
M Garbarg et al. S-[2-(4-Imidazolyl)ethyl]isothiourea, a highly specific and potent histamine H3 receptor agonist. J. Pharmacol. Exp. Ther. 1992, 263, 304.
Certificate of Analysis
Material Safety Data Sheet
CNS
Diabetes & Metabolism
Immunology
Pain & Inflammation
H3
A18
H3 agonist
Chemical name
2-[2-(1H-Imidazol-4-yl)-ethyl]-isothiourea dihydrobromide
Parent CAS No.
[102203-18-9]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| Dimaprit dihydrochloride | Axon 1324
CAS [23256-33-9]
MF C6H15N3S.2HClMW 234.19
Purity:
98%
No solubility data
Description
Standard histamine H2 receptor agonist
References
Certificates
Categories
Extra info
Paquayet al. Nitric oxide synthase inhibition by dimaprit and dimaprit analogues. Br. J. Pharmacol. 1999, 127, 331.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Immunology
Pain & Inflammation
H2
A18
H2 agonist
Chemical name
2-(3-Dimethylamino-propyl)-isothiourea dihydrochloride
Parent CAS No.
[65119-89-3]
Order
Size
Unit Price
Stock
10 mg
€45.00
In Stock | | axonmedchem |
| JNJ 7777120 | Axon 1306
CAS [459168-41-3]
MF C14H16ClN3OMW 277.75
Purity:
99%
Soluble in DMSO and Ethanol
Description
First potent and selective non-imidazole histamine H4 antagonist
References
Certificates
Categories
Extra info
H Xie et al. AST1306, A Novel Irreversible Inhibitor of the Epidermal Growth Factor Receptor 1 and 2, Exhibits Antitumor Activity Both In Vitro and In Vivo. PLoS ONE 2011, 6(7), e21487.
Certificate of Analysis
Material Safety Data Sheet
CNS
Immunology
Pain & Inflammation
H4
A18
H4 antagonist
Chemical name
(5-Chloro-1H-indol-2-yl)-(4-methyl-piperazin-1-yl)-methanone
Parent CAS No.
[459168-41-3]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| Loratadine - SCH 29851 | Axon 1299
CAS [79794-75-5]
MF C22H23ClN2O2MW 382.88
Purity:
99%
Soluble in Ethanol
Description
Histamine H1 receptor antagonist; non-sedating antihistamine, used as a drug to treat allergies
References
Certificates
Categories
Extra info
Barnett et al. Evaluation of the CNS properties of SCH 29851, a potential non-sedating antihistamine. Agents Actions. 1984, 14, 590.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Immunology
Pain & Inflammation
H1
A18
H1 antagonist
Chemical name
4-(8-Chloro-5,6-dihydro-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-piperidine-1-carboxylic acid ethyl ester
Parent CAS No.
[79794-75-5]
Order
Size
Unit Price
Stock
10 mg
€70.00
In Stock | | axonmedchem |
| Clobenpropit dihydrobromide - VUF 9153 dihydrobromide | Axon 1209
CAS [145231-35-2]
MF C14H17ClN4S.2HBrMW 470.65
Purity:
99%
Soluble in water
Description
Potent histamine H3 receptor antagonist
References
Certificates
Categories
Extra info
Yokoyamaet al. Clobenpropit (VUF-9153), a new histamine H3 receptor antagonist, inhibits electrically induced convulsions in mice. Eur. J. Pharmacol. 1994, 260, 23.
Certificate of Analysis
Material Safety Data Sheet
CNS
Diabetes & Metabolism
Immunology
Pain & Inflammation
H3
A18
H3 antagonist
Chemical name
1-(4-Chloro-benzyl)-2-[3-(1H-imidazol-4-yl)-propyl]-isothiourea dihydrobromide
Parent CAS No.
[145231-45-4]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| UNC 0224 | Axon 1789
CAS [1197196-48-7]
MF C26H43N7O2MW 485.67
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent and selective inhibitor of G9a histone lysine methyltransferase (HMTase) (IC50: 15 nM)
References
Certificates
Categories
Extra info
F Liu et al. Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a. J. Med. Chem. 2009, 52(24), 7950-7953.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
EC 2.1.1.43
HMTase
Inhibitor of G9a HMTase
Chemical name
7-(3-(dimethylamino)propoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
Parent CAS No.
[1197196-48-7]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| Methylhistamine dihydrochloride, 4- | Axon 1261
CAS [36376-47-3]
MF C6H11N3.2HClMW 198.09
Purity:
98%
Soluble in water and DMSO
Description
Potent and selective histamine H4 agonist
References
Certificates
Categories
Extra info
RK Morgan et al. Histamine 4 receptor activation induces recruitment of FoxP3+ T cells and inhibits allergic asthma in a murine model. J. Immunol. 2007, 178(12), 8081-9.
Dijkstra, D. et al. Histamine downregulates monocyte CCL2 production through the histamine H4 receptor. J Allergy Clin Immunol. 2007, 120(2), 300-7.
Lim et al. Evaluation of histamine H1- H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J. Pharmacol. Exp. Ther. 2005, 314, 1310.
Certificate of Analysis
Material Safety Data Sheet
CNS
Immunology
Pain & Inflammation
H4
A18
H4 agonist
Chemical name
2-(5-Methyl-1H-imidazol-4-yl)-ethylamine dihydrochloride
Parent CAS No.
[36507-31-0]
Order
Size
Unit Price
Stock
10 mg
€115.00
In Stock | | axonmedchem |
| Amthamine dihydrobromide | Axon 1207
CAS [142457-00-9]
MF C6H11N3S.2HBrMW 319.06
Purity:
99%
Soluble in water
Description
Standard selective histamine H2 agonist
References
Certificates
Categories
Extra info
CI Ezeamuzie et al. Histamine H2 receptors mediate the inhibitory effect of histamine on human eosinophil degranulation. Br. J. Pharmacol. 2000, 131, 482-488.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Immunology
Pain & Inflammation
H2
A18
H2 agonist
Chemical name
5-(2-Amino-ethyl)-4-methyl-thiazol-2-ylamine dihydrobromide
Parent CAS No.
[142437-67-0]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| DG2 - S6K1 Inhibitor DG2 | Axon 1903
CAS [871340-88-4]
MF C16H17BrN6OMW 389.25
Purity:
99%
Soluble in DMSO
Description
Potent and selective inhibitor of p70 ribosomal S6 kinase 1 (S6K1) (IC50: 9.1 nM for S6K1); no Akt activity (IC50: 22000 nM); ATP-competitive and cell-permeable
References
Certificates
Categories
Extra info
T Okuzumi et al. Inhibitor Hijacking of Akt Activation. Nat. Chem. Biol. 2009, 5(7), 484–493.
BT Wang et al. The mammalian target of rapamycin regulates cholesterol biosynthetic gene expression and exhibits a rapamycin-resistant transcriptional profile. PNAS 2011, 108 (37), 15201-15206.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
MAPK
PI3K-Akt-mTOR
EC 2.7.11.1
p70-RSK
RSK inhibitor (p70 ribosomal S6 kinase 1 specific)
Chemical name
3-bromo-4-(4-(2-methoxyphenyl)piperazin-1-yl)-1H-pyrazolo[3,4-d]pyrimidine
Parent CAS No.
[871340-88-4]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| AZD 5363 dihydrochloride - Capivasertib | Axon 1859
CAS [2108875-84-7]
MF C21H25ClN6O2.2HClMW 501.84
Purity:
99%
Soluble in water and DMSO
Description
Orally bioavailable, selective and potent protein kinase B (Akt) inhibitor in low nM potency; AZD5363 dihydrochloride is directly water-soluble.
KEYWORDS: AZD 5363 dihydrochloride | supplier | Akt inhibitor | Capivasertib | AZD5363 | AZD-5363 | CAS [1143532-39-1] | Axon Medchem | Axon 1859 | Phosphatidylinositol | Akt | Inhibitor | Enzymes | | axonmedchem |
| PHT 427 | Axon 1870
CAS [1191951-57-1]
MF C20H31N3O2S2MW 409.61
Purity:
99%
Soluble in DMSO
Description
Inhibitor of AKT and phosphoinositide-dependent protein kinase 1 (PDPK1 or PDK1). PH 427 binds to the pleckstrin homology (PH) domain of Akt and PDPK1 signaling with significant in vivo antitumor activity and minimal toxicity
References
Certificates
Categories
Extra info
EJ Meuillet et al. Molecular Pharmacology and Antitumor Activity of PHT-427, a Novel Akt/Phosphatidylinositide-Dependent Protein Kinase 1 Pleckstrin Homology Domain Inhibitor. Mol. Cancer Ther. 2010, 9, 706.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Akt
PI3K-Akt-mTOR
EC 2.7.11.1
PDPK
Inhibitor of Akt and PDPK1
Chemical name
4-dodecyl-N-(1,3,4-thiadiazol-2-yl)benzenesulfonamide
Parent CAS No.
[1191951-57-1]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| GSK 690693 | Axon 1729
CAS [937174-76-0]
MF C21H27N7O3MW 425.48
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent and ATP-competitive Akt kinase inhibitor, with IC50 to be 2, 13 and 9 nM for Akt1, Akt2 and Akt3 respectively
References
Certificates
Categories
Extra info
N Rhodes et al. Characterization of an Akt Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity. Cancer Res. 2008, 68(7), 2366-2374.
DA Heerding et al. Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase. J. Med. Chem. 2008, 51(18), 5663-5679.
DS Lew et al. AKT inhibitor, GSK690693, induces growth inhibition and apoptosis in acute lymphoblastic leukemia cell lines. Blood. 2009, 113(8), 1723-1729.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Akt
PI3K-Akt-mTOR
EC 2.7.11.1
ATP-competitive pan-Akt kinase inhibitor
Chemical name
(S)-4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-(piperidin-3-ylmethoxy)-1H-imidazo[4,5-c]pyridin-4-yl)-2-methylbut-3-yn-2-ol
Parent CAS No.
[937174-76-0]
Order
Size
Unit Price
Stock
5 mg
€115.00
In Stock | | axonmedchem |
| SC 66 | Axon 1790
CAS [871361-88-5]
MF C18H16N2OMW 276.33
Purity:
99%
Soluble in DMSO and Ethanol
Description
An allosteric Akt inhibitor, targeting pleckstrin homology domain and facilitating Akt ubiquitination
References
Certificates
Categories
Extra info
J Hakryul et al. Deactivation of Akt by a small molecule inhibitor targeting pleckstrin homology domain and facilitating Akt ubiquitination. Proc. Natl. Acad. Sci. USA 2011, 108(16), 6486-6491.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Akt
PI3K-Akt-mTOR
Ubiquitin
EC 2.7.11.1
Allosteric Akt inhibitor
Chemical name
(2E,6E)-2,6-bis(pyridin-4-ylmethylene)cyclohexanone
Parent CAS No.
[871361-88-5]
Order
Size
Unit Price
Stock
10 mg
€70.00
In Stock | | axonmedchem |
| MK 2206 | Axon 1684
CAS [1032350-13-2]
MF C25H21N5O.2HClMW 480.39
Purity:
99%
Soluble in water and DMSO
Description
An orally potent and highly selective non-ATP-competitive allosteric Akt inhibitor that has nanomolar IC50 values and broad preclinical anti-tumor activities.
KEYWORDS: MK 2206 | Akt inhibitor | MK2206 | MK-2206 | CAS [1032350-13-2] | [1032349-93-1] | Axon Medchem | Axon 1684 | Phosphatidylinositol | Akt | Inhibitor | Enzymes | | axonmedchem |
| YS 49 | Axon 1685
CAS [132836-42-1]
MF C20H19NO2.HBrMW 386.28
Purity:
98%
Soluble in DMSO
Description
Anti-inflammatory agent; Antithrombotic; Antiplatelet; YS-49 protects cells from oxidant injury; induces heme oxygenase (HO-1) in endothelial cells and protects cells from oxidant injury; activator of PI3K/Akt signaling
References
Certificates
Categories
Extra info
HS Yun-Choi et al. Antithrombotic Effects of YS-49 and YS-51—1-Naphthylmethyl Analogs of Higenamine. Thromb. Res. 2001, 104(4), 249-255.
MK Pyo et al. Effects of two tetrahydroisoquinolines (YS-49 and YS-51) on experimental disseminated intravascular coagulation induced by lipopolysaccharide in rats. Arzneimittelforschung. 2004, 54(11), 705-10.
K Tsoyi et al. HO-1 and JAK-2/STAT-1 signals are involved in preferential inhibition of iNOS over COX-2 gene expression by newly synthesized tetrahydroisoquinoline alkaloid, CKD712, in cells (...). Cell Signal. 2008, 20, 1839-47.
JJ Sun, et al, YS-49, 1-(a-naphthylmethyl)-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline, regulates angiotensin II-stimulated ROS production, JNK phosphorylation and vascular smooth muscle cell proliferation (...). Life Sci. 2008, 82, 600-607.
M. K. Pyo et al. Effects of higenamine and its 1-nahthyl analogs, YS-49 and YS-51, on platelet TXA2 synthesis and aggregation, Thromb. Res. 2007, 120, 81-86.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
Pain & Inflammation
Akt
PI3K-Akt-mTOR
EC 2.7.11.1
Antiplatelet, antithrombotic
Chemical name
1-(naphthalen-1-ylmethyl)-1,2,3,4-tetrahydroisoquinoline-6,7-diol hydrobromide
Parent CAS No.
[132836-11-4]
Order
Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| PF 4708671 - PF 04708671 | Axon 1602
CAS [1255517-76-0]
MF C19H21F3N6MW 390.41
Purity:
99%
Soluble in DMSO
Description
Highly specific and cell-permeable p70 ribosomal S6 kinase (S6K1) inhibitor with Ki of 20 nM and IC50 of 160 nM; having no effect on the closely related RSK and MSK kinases; Useful tool for delineating S6K1-specific roles downstream of mTOR
References
Certificates
Categories
Extra info
LR Pearce et al. Characterisation of PF-4708671 a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1). Biochem. J. 2010, 431, 245-255.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
MAPK
PI3K-Akt-mTOR
EC 2.7.11.1
p70-RSK
Pfizer Licensed Products
RSK inhibitor (p70 RSK specific)
Chemical name
2-((4-(5-ethylpyrimidin-4-yl)piperazin-1-yl)methyl)-5-(trifluoromethyl)-1H-benzo[d]imidazole
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[1255517-76-0]
Order
Size
Unit Price
Stock
10 mg
€110.00
In Stock | | axonmedchem |
| Perifosine - KRX 0401 | D 21266 | Axon 1663
CAS [157716-52-4]
MF C25H52NO4PMW 461.66
Purity:
98%
Soluble in water
Description
Orally available Akt inhibitor that inhibits Akt activation in the PI3K pathway
References
Certificates
Categories
Extra info
JJ Gills and PA Dennis. Perifosine: update on a novel Akt inhibitor. Curr. Oncol. Rep. 2009, 11(2), 102-110.
SB Kondapaka et al. Perifosine, a novel alkylphospholipid, inhibits protein kinase B activation. Mol. Cancer Ther. 2003, 2(11), 1093-1103.
V Patel et al. Perifosine, a novel alkylphospholipid, induces p21(WAF1) expression in squamous carcinoma cells through a p53-independent pathway, leading to loss in cyclin-dependent kinase activity (...). Cancer Res. 2002, 062(5), 1401-1409.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Akt
PI3K-Akt-mTOR
EC 2.7.11.1
PI3K/Akt inhibitor
Chemical name
1,1-dimethylpiperidinium-4-yl octadecyl phosphate
Parent CAS No.
[157716-52-4]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| GSK 650394 | Axon 1570
CAS [890842-28-1]
MF C25H22N2O2MW 382.45
Purity:
99%
Soluble in DMSO
Description
Specific inhibitor of serum- and glucocorticoid-regulated kinases 1 (SGK 1), with IC50 values to be 62 and 103 nM for SGK1 and SGK2 respectively
References
Certificates
Categories
Extra info
AB Sherk et al. Development of a small molecule serum and glucocorticoid-regulated kinase 1 antagonist and its evaluation as a prostate cancer therapeutic. Cancer Res. 2008, 68(18), 7475–7483.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
Pain & Inflammation
Endocrinology
EC 2.7.11.1
SGK
SGK1 Inhibitor
Chemical name
2-Cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-benzoic acid
Parent CAS No.
[890842-28-1]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| Deguelin | Axon 1239
CAS [522-17-8]
MF C23H22O6MW 394.42
Purity:
98%
Soluble in DMSO and Ethanol
Description
Inhibitor of activated Akt. Anticancer, chemopreventive agent
References
Certificates
Categories
Extra info
AS Nair et al. Deguelin, an Akt Inhibitor, Suppresses IKBa Kinase Activation Leading to Suppression of NF-KB-Regulated Gene Expression, Potentiation of Apoptosis, and Inhibition of Cellular Invasion. J. Immunol. 2006, 177, 5612-5622.
KH Chun et al. Effects of deguelin on the phosphatidylinositol 3-kinase/Akt pathway and apoptosis in premalignant human bronchial epithelial cells. J. Natl. Cancer Inst. 2003, 95, 291-302.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Akt
PI3K-Akt-mTOR
EC 2.7.11.1
Akt inhibitor
Chemical name
(7aS,13aS)-9,10-Dimethoxy-3,3-dimethyl-13,13a-dihydro-3H,7aH-pyrano[2,3-c;6,5-f']dichromen-7-one
Parent CAS No.
[522-17-8]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| GSK 269962A - GSK 269962 | Axon 1167
CAS [850664-21-0]
MF C29H30N8O5MW 570.60
Purity:
99%
Soluble in DMSO
Description
Highly potent and selective inhibitor of Rho-Kinase (ROCK), with IC50 values: 1.6 nM toward ROCK1 and 6 nM toward ROCK2 and high kinase selectivity (>30 fold selective for ROCK compared to other protein kinases tested) and with antihypertensive activity; cardiovascular diseases category. GSK269962A has a much improved potency and selectivity in comparison with Y-27632, which has IC50 values of 140-220 nM for ROCK1 and ROCK2
References
Certificates
Categories
Extra info
C Doe et al. Novel Rho Kinase Inhibitors with Anti-inflammatory and Vasodilatory Activities. J. Pharmacol. Exp. Ther. 2007, 320, 89-98.
D Schaafsma et al. Rho kinase inhibitors: A novel therapeutical intervention in asthma? Eur. J. Pharmacol. 2008, 585(2-3), 398-406.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Stem Cell
ROCK
TGF-β
EC 2.7.11.1
ROCK1 and ROCK2 inhibitor
Chemical name
N-{3-[2-(4-Amino-furazan-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-6-yloxy]-phenyl}-4-(2-morpholin-4-yl-ethoxy)-benzamide
Parent CAS No.
[850664-21-0]
Order
Size
Unit Price
Stock
2 mg
€65.00
In Stock | | axonmedchem |
| Thiazovivin - TZV | Axon 1535
CAS [1226056-71-8]
MF C15H13N5OSMW 311.36
Purity:
99%
Soluble in DMSO
Description
A small molecule that enhances the survival of human embryonic stem cells (hESCs) after trypsinzation; ROCK inhibitor; Thiazovivin dramatically improves (200-fold) the efficiency of iPSC generation from human fibroblasts, when used in combination with ALK5 inhibitor SB 431542 (Axon 1661) and MEK inhibitor PD 0325091 (Axon 1408)
*Promotion | | axonmedchem |
| LY 2784544 - Gandotinib | Axon 2554
CAS [1229236-86-5]
MF C23H25ClFN7OMW 469.94
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent, selective and ATP-competitive inhibitor of janus kinase 2 (JAK2) tyrosine kinase (IC50 value 20 and 55 nM for inhibition of JAK2V617F-driven signaling and cell proliferation in Ba/F3 cells, respectively), with no significant inhibitory effect on IL-3 stimulated wild-type JAK2-mediated signaling and cell proliferation (IC50 values >1180 nM) A selective tool for suppression of JAK2V617F-induced myeloproliferative neoplasm (MPN) pathogenesis while minimizing effects on hematopoietic progenitor cells. Moreover, LY2784544 induced apoptosis in inflammatory breast cancer spheres through targeting IL-6-JAK-STAT3 pathway; tested positive in Phase I study in patients with myelofibrosis (MF), polycythemia vera (PV), and essential thrombocythemia (ET).
KEYWORDS: LY 2784544 | supplier | JAK2 Inhibitor | Gandotinib | LY2784544 |CAS [1229236-86-5] | JAK-STATPathway | JAK | Inhibitor | janus kinase | tyrosine kinase | ATP competitive | JAK2V617F | proliferation | myeloproliferative neoplasm | MNP | apoptosis | inflammatory | myelofibrosis (MF) | polycythemia vera (PV) | essential thrombocythemia (ET) | | axonmedchem |
| VX 770 - Ivacaftor | Kalydeco | Axon 2503
CAS [873054-44-5]
MF C24H28N2O3MW 392.49
Purity:
99%
Soluble in DMSO
Description
Orally bioavailable CFTR potentiator; FDA-approved drug for clinical application to patients with cystic fibrosis (CF). VX770 enhances spontaneous, ATP-independent activity of WT-CFTR to a similar magnitude as its effects on G551D channels.
KEYWORDS: VX 770 | supplier | CFTR potentiator | Ivacaftor | Kalydeco | VX770 | [873054-44-5] | [1174930-71-2] | Ion Channel | Cystic Fibrosis | CF | FDA-approved | ATP-independent | | axonmedchem |
| IN 1130 | Axon 2236
CAS [868612-83-3]
MF C25H20N6OMW 420.47
Purity:
99%
Soluble in DMSO
Description
Highly selective small molecule ALK5 inhibitor (IC50 value of 5.3 nM for inhibition of ALK5-mediated Smad3 phosphorylation) with >100 fold selectivity over p38α and a panel of 26 other serine/threonine and tyrosine kinases. Suppressor of fibrogenic process of unilateral ureteral obstruction in rats underscoring the potential clinical benefits in the treatment of renal fibrosis. By inhibition of TGF-β signaling, IN1130 ameliorated experimental autoimmune encephalomyelitis, lessened tunical fibrosis and corrected penile curvature in rats, inhibited cancer metastasis in MMTV/c-Neu breast cancer mice, and enhanced CTL response in cancer mice.
References
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C.Y. Park et al. An novel inhibitor of TGF-β type I receptor, IN-1130, blocks breast cancer lung metastasis through inhibition of epithelial-mesenchymal transition. Cancer Lett. 2014 Aug 28;351(1):72-80.
C.H. Jin et al. Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors. Bioorg Med Chem. 2011 Apr 15;19(8):2633-40.
J.A. Moon et al. IN-1130, a novel transforming growth factor-bold italic beta type I receptor kinase (ALK5) inhibitor, suppresses renal fibrosis in obstructive nephropathy. Kidney International (2006) 70, 1234–1243.
G.T. Lee et al. Effect of IN-1130, a small molecule inhibitor of transforming growth factor-beta type I receptor/activin receptor-like kinase-5, on prostate cancer cells. J Urol. 2008 Dec;180(6):2660-7.
J.K. Ryu et al. IN-1130, a novel transforming growth factor-beta type I receptor kinase (activin receptor-like kinase 5) inhibitor, promotes regression of fibrotic plaque and corrects penile curvature.... J Sex Med. 2009 May;6(5):1284-96.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Stem Cell
TGF-β
RSTK class I; EC 2.7.11.30
TGF-βR
TGF-βR 1 inhibitor
Chemical name
3-((5-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)-1H-imidazol-2-yl)methyl)benzamide
Parent CAS No.
[868612-83-3]
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Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| Pexidartinib - PLX 3397 | Axon 2501
CAS [1029044-16-3]
MF C20H15ClF3N5MW 417.81
Purity:
99%
Soluble in DMSO
Description
Multi-targeted receptor tyrosine kinase inhibitor of CSF1R, c-Kit, and FLT3 (IC50 values 13 nM, 27 nM, and 11 nM, respectively) Administration of PLX3397 reduced CIBP, induced substantial intratumoral fibrosis, and was also highly efficacious in reducing tumor cell growth, formation of new tumor colonies in bone, and pathological tumor-induced bone remodeling. PLX3397 is superior to imatinib in the treatment of malignant peripheral nerve sheath tumor (MPNST), and the combination of PLX3397 with a TORC1 inhibitor could provide a new therapeutic approach for the treatment of this disease.
KEYWORDS: Pexidartinib | supplier | RTK inhibitor | PLX 3397 | PLX3397 | CAS [1029044-16-3] | FLT3LG | FLT3 | c-KIT | CSF1R | cytokine | tyrosine kinase | CIBP | MPNST | TORC1 | cluster of differentiation | hematopoietic | stem cell factor | SCF | | axonmedchem |
| AM 095 (parent compound) | Axon 2367
CAS [1228690-36-5]
MF C27H24N2O5MW 456.49
Purity:
99%
Optical purity:
Optically pure
Soluble in 0.1N NaOH(aq) and DMSO
Description
A novel potent and selective LPA1 antagonist (IC50 values 0.025 μM and 0.023 μM for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells,respectively). AM 095 attenuates bleomycin-induced dermal fibrosis.
References
Certificates
Categories
Extra info
F.V. Castelino et al. Genetic deletion or pharmacologic antagonism of LPA1 ameliorates dermal fibrosis in a scleroderma mouse model. Arthritis Rheum. 2011, 63, 1405-1415.
Certificate of Analysis
Material Safety Data Sheet
Pain & Inflammation
A13
LPA1
Novel potent and selective LPA1 antagonist
Chemical name
(R)-2-(4'-(3-methyl-4-((1-phenylethoxy)carbonylamino)isoxazol-5-yl)biphenyl-4-yl)acetic acid
Parent CAS No.
[1228690-36-5]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| GW 311616A - GW 311616 hydrochloride | Axon 2364
CAS [197890-44-1]
MF C19H31N3O4S.HClMW 433.99
Purity:
99%
Optical purity:
>99% ee
Soluble in water and DMSO
Description
Potent, selective and orally active human neutrophil elastase (HNE) inhibitor (IC50 value 22 nM). GW311616A is selective over other human serine proteases (IC50 values >100 μM for trypsin, cathepsin G, and plasmin, >3 μM for chymotrypsin and tissue plasminogen activator), and does not inhibit AchE at 100 μM.
References
Certificates
Categories
Extra info
S.J. Macdonald et al. The discovery of a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase--GW311616A a development candidate. Bioorg Med Chem Lett. 2001 Apr 9;11(7):895-8.
J.W. Cooke et al. A novel and selective approach to enantiomerically pure bicyclic-trans-lactams via a titanium enolate of a thiopyridyl ester. J Org Chem. 2001 Jan 12;66(1):334-6.
S.J.F. Macdonald et al. A flexible, practical, and stereoselective synthesis of enantiomerically pure trans-5-oxohexahydropyrrolo[3,2-b]pyrroles (pyrrolidine-trans-lactams), a new class of serine protease....J.O.C. 1999 June 17, 64(14), 5166-5175.
V. Papayannopoulos et al. Neutrophil elastase enhances sputum solubilization in cystic fibrosis patients receiving DNase therapy. PLoS One. 2011;6(12):e28526.
Certificate of Analysis
Material Safety Data Sheet
Immunology
Miscellaneous
Pain & Inflammation
EC 3.4.21.37
HNE
Potent, selective and orally active human neutrophil elastase (HNE) inhibitor
Chemical name
(3S,3aS,6aR)-3-isopropyl-1-(methylsulfonyl)-4-((E)-4-(piperidin-1-yl)but-2-enoyl)hexahydropyrrolo[3,2-b]pyrrol-2(1H)-one hydrochloride
Parent CAS No.
[198062-54-3]
Order
Size
Unit Price
Stock
2 mg
€135.00
In Stock | | axonmedchem |
| VX 661 - Tezacaftor | Axon 2169
CAS [1152311-62-0]
MF C26H27F3N2O6MW 520.50
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Corrector of the cystic fibrosis transmembrane conductance regulator (CFTR), hypothesized to restore F508del mutation processing and plasma membrane localization of CFTR protein, thereby effectively increasing functional surface CFTR ion channels. VX 661 is the second CFTR corrector in line with VX 809 (first), and VX 983 (third), and is believed to help CFTR protein reach the cell surface.
Tested in phase 2 to evaluate safety, efficacy, pharmacokinetics, and pharmacodynamics in subjects with cystic fibrosis suffering from the F508del-CFTR mutation.
References
Certificates
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Extra info
Vertex Pharmaceuticals Incorporated. Study of VX-661 Alone and in Combination With VX-770 in Subjects Homozygous to the F508del-CFTR Mutation. ClinicalTrials.gov [Online]. 2012.
A. Opar. Excitement mounts for first disease-modifying cystic fibrosis drugs. Nat. Rev. Drug. Discov. 2011, 10, 479-480.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CFTR
EC 3.6.3.49
Corrector of the cystic fibrosis transmembrane conductance regulator (CFTR)
Chemical name
(R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide
Parent CAS No.
[1152311-62-0]
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Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| PPQ 102 | Axon 2295
CAS [931706-15-9]
MF C26H22N4O3MW 438.48
Purity:
99%
Soluble in DMSO
Description
Potent CFTR inhibitor (IC50 value ca 90 nM in CFTR chloride conductance essay). PPQ 102 acts by a mechanism involving stabilization of the channel closed-state. Prevented cyst expansion and reduced the size of preformed cysts in an embryonic kidney organ culture model of Polycystic kidney disease (PKD).
References
Certificates
Categories
Extra info
L. Tradtrantip et al. Nanomolar potency pyrimido-pyrrolo-quinoxalinedione CFTR inhibitor reduces cyst size in a polycystic kidney disease model. J. Med. Chem. 2009, 52, 6447-6455.
D.S. Snyder et al. Potent, metabolically stable benzopyrimido-pyrrolo-oxazine-dione (BPO) CFTR inhibitors for polycystic kidney disease. J. Med. Chem. 2011, 54, 5468-5477.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CFTR
EC 3.6.3.49
CFTR inhibitor that acts by a mechanism involving stabilization of the channel closed-state
Chemical name
6,7-dihydro-7,9-dimethyl-6-(5-methyl-2-furanyl)-11-phenyl-pyrimido[4',5':3,4]pyrrolo[1,2-a]quinoxaline-8,10(5H,9)-dione
Parent CAS No.
[931706-15-9]
Order
Size
Unit Price
Stock
5 mg
€100.00
In Stock | | axonmedchem |
| TY 52156 | Axon 2404
CAS [934369-14-9]
MF C18H19Cl2N3OMW 364.27
Purity:
99%
Soluble in DMSO
Description
Selective, competitive, and orally active S1P3 antagonist that restores S1P reduced coronary blood flow, and inhibits Rho dependent activation and calcium signaling. TY52156 inhibited FTY720-induced S1P3 receptor-mediated bradycardia in vivo.
References
Certificates
Categories
Extra info
A. Murakami et al. Sphingosine 1-phosphate (S1P) regulates vascular contraction via S1P3 receptor: investigation based on a new S1P3 receptor antagonist. Mol Pharmacol. 2010 Apr;77(4):704-13.
N.J. Pyne et al. Selectivity and specificity of sphingosine 1-phosphate receptor ligands: "off-targets" or complex pharmacology? Front Pharmacol. 2011 May 31;2:26.
K. Sobel et al. Sphingosine 1-phosphate (S1P) receptor agonists mediate pro-fibrotic responses in normal human lung fibroblasts via S1P2 and S1P3 receptors and Smad-independent signaling. J Biol Chem. 2013 May 24;288(21):14839-51.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Apoptosis
Cardiovascular
Immunology
Miscellaneous
A13
S1PR3
Selective, competitive, and orally active S1P3 antagonist
Chemical name
N,N'-bis(4-chlorophenyl)-3,3-dimethyl-2-oxobutanehydrazonamide
Parent CAS No.
[934369-14-9]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| BAY-678 | Axon 2822
CAS [675103-36-3]
MF C20H15F3N4O2MW 400.35
Purity:
99%
Optical purity:
99% ee
Soluble in DMSO
Recently added | | axonmedchem |
| Odiparcil - SB 424323 | GSK 424323 | Axon 1536
CAS [137215-12-4]
MF C15H16O6SMW 324.35
Purity:
99%
Soluble in DMSO
Description
Orally active anti-thrombotic agent under clinical development, with limited hemorrhagic risk and a unique mechanism of action involving the induction of glycosaminoglycans (GAGs) biosynthesis; indirect thrombin inhibitor (via. Heparin cofactor II)
References
Certificates
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Extra info
JR Toomey et al. A comparison of the β-D-xyloside, odiparcil, to warfarin in a rat model of venous thrombosis. J. Thrombosis and Haemostasis 2006, 4(9), 1989-1996.
VV Upreti et al. Determination of endogenous glycosaminoglycans derived disaccharides in human plasma by HPLC: Validation and application in a clinical study. J. Chromatography B. 2006, 831 (1-2), 156-162.
BI Eriksson and DJ Quinlan. Oral anticoagulants in development: focus on thromboprophylaxis in patients undergoing orthopaedic surgery. Drugs. 2006, 66(11), 1411-29.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
EC 3.4.21.5
Heparine CoF II
Thrombin inhibitor (via Heparin CoFII)
Chemical name
7-((2R,3R,4S,5S)-tetrahydro-3,4,5-trihydroxy-2H-thiopyran-2-yloxy)-4-methyl-2H-chromen-2-one
Parent CAS No.
[137215-12-4]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| TM 5275 | Axon 2344
CAS [1103926-82-4]
MF C28H27ClN3NaO5MW 543.97
Purity:
99%
Soluble in DMSO
Description
Selective, orally active inhibitor of plasminogen activator inhibitor-1 (PAI-1; IC50 value 6.95 µM in tissue plasminogen activator-dependent peptide hydrolysis essay) with antithrombotic benefits devoid of bleeding effect in rodents and nonhuman primates, and with impressive bioavailability.TM 5275 prolongs tPA retention and enhances plasmin generation on the vascular endothelial cell (VEC) surface as a result of PAI-1 inhibition.Additionally, TM 5275 represents a novel class of anti-inflammatory agents targeting macrophage migration by the inhibition of the interaction of PAI-1 with low-density lipoprotein receptor–related protein (IC50 values 3.13 µM and 3.02 µM for LRP1 protein Cl II and Cl IV, respectively).
References
Certificates
Categories
Extra info
Y. Izuhara et al. A novel inhibitor of plasminogen activator inhibitor-1 provides antithrombotic benefits devoid of bleeding effect in nonhuman primates. J. Cereb. Blood Flow Metab. 2010, 30, 904-912.
H. Yasui et al. TM5275 prolongs secreted tissue plasminogen activator retention and enhances fibrinolysis on vascular endothelial cells. Thromb. Res. 2013, 132, 100-105.
A. Ichimura et al. A small molecule inhibitor to plasminogen activator inhibitor 1 inhibits macrophage migration. Arterioscler. Thromb. Vasc. Biol. 2013, 33, 935-942.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
Miscellaneous
Pain & Inflammation
Plasminogen activator inhibitor-1 (PAI-1)
EC 3.4.21
Selective and orally active inhibitor of PAI-1
Chemical name
Sodium 2-(2-(2-(4-benzhydrylpiperazin-1-yl)-2-oxoethoxy)acetamido)-5-chlorobenzoate
Parent CAS No.
[1103928-13-7]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| PF 543 citrate | Axon 2350
CAS [1415562-83-2]
MF C27H31NO4S.C6H8O7MW 657.73
Purity:
98%
Optical purity:
Optically pure
Soluble in water and DMSO
Description
Cell-permeant reversible inhibitor of SphK1 (IC50 value 2.0 nM; Ki value 3.6 nM). PF-543 is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform.
References
Certificates
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Extra info
D. Vogt et al. Design, synthesis and evaluation of 2-aminothiazole derivatives as sphingosine kinase inhibitors. Bioorg. Med. Chem. 2014, 22, 5354-5367.
M.E. Schnute et al. Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1. Biochem. J. 2012, 444, 79-88.
J. Wang et al. Crystal Structure of Sphingosine Kinase 1 with PF-543. ACS Med Chem Lett. 2014, 5, 1329-1333.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Apoptosis
Cell Signaling & Oncology
Immunology
Miscellaneous
Pain & Inflammation
EC 2.7.1.91
SphK
Pfizer Licensed Products
Cell-permeant reversible inhibitor of SphK1
Chemical name
(R)-(1-(4-((3-methyl-5-(phenylsulfonylmethyl)phenoxy)methyl)benzyl)pyrrolidin-2-yl)methanol 2-hydroxypropane-1,2,3-tricarboxylate
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[1415562-82-1]
Order
Size
Unit Price
Stock
5 mg
€99.00
In Stock | | axonmedchem |
| K 145 hydrochloride | Axon 2235
CAS [1449240-68-9]
MF C18H24N2O3S.HClMW 384.92
Purity:
99%
Soluble in water and DMSO
Description
Selective, substrate competitive Sphingosine Kinase-2 inhibitor (SphK2; IC50 value 4.30 µM) and anticancer agent. K145 suppressed the S1P level, and significantly inhibited the growth of U937 tumors in nude mice by both intraperitoneal and oral administration.K145 significantly inhibited the phosphorylation of FTY720, ERK and Akt upon treatment of U937 cells, but does not interfere with CERK and/or ceramide synthase.
References
Certificates
Categories
Extra info
K. Liu et al. Biological characterization of 3-(2-amino-ethyl)-5-[3-(4-butoxyl-phenyl)-propylidene]-thiazolidine-2,4-dione (K145) as a selective sphingosine kinase-2 inhibitor and anticancer agent. PLoS One. 2013, 8, e56471.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Apoptosis
Cell Signaling & Oncology
Immunology
Miscellaneous
EC 2.7.1.91
SphK
Selective, substrate competitive SphK2 inhibitor
Chemical name
3-(2-aminoethyl)-5-(3-(4-butoxyphenyl)propylidene)thiazolidine-2,4-dione hydrochloride
Parent CAS No.
[1309444-75-4]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| TM 5441 | Axon 2734
CAS [1190221-43-2]
MF C21H17ClN2O6MW 428.82
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
TM5441 is an orally active PAI-1 inhibitor, which protects mice against L-NAME–induced vascular pathologies, including hypertension, fibrosis, and vascular senescence. TM5441 is a derivative of PAI-1 inhibitor TM5275 (Axon 2344), however showed better pharmacokinetics and volume of distribution.
KEYWORDS: TM 5441 | supplier | PAI-1 inhibitor | TM-5441 | TM5441 | CAS [1190221-43-2] | Serpin | Plasminogen activator inhibitor-1 (PAI-1) | Inhibitor | Enzymes | L-NAME | | axonmedchem |
| T 1776Na | Axon 1769
CAS [1202075-60-2]
MF C25H18NNaO4MW 419.40
Purity:
99%
Poorly soluble in DMSO
Description
Inhibitor of plasminogen activator inhibitor-1 (PAI-1)
References
Certificates
Categories
Extra info
H Miyazaki et al. Synthesis and Evaluation of Pyrrolin-2-one Compounds, a Series of Plasminogen Activator Inhibitor-1 Inhibitors. Chem. Pharm. Bull. 2009, 57(9), 979-985.
H Miyazaki et al. Evaluation of pyrrolin-2-one derivatives synthesized by a new practical method as inhibitors of plasminogen activator inhibitor-1 (PAI-1). Bioorg. Med. Chem. Lett. 2010, 20(2), 546-548.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Miscellaneous
Plasminogen activator inhibitor-1 (PAI-1)
EC 3.4.21
Inhibitor of plasminogen activator inhibitor-1
Chemical name
sodium (Z)-2-(3-((5-oxo-3,4-diphenyl-1H-pyrrol-2(5H)-ylidene)methyl)phenyloxo-3,4-diphenyl-1H-pyrrol-2(5H)-ylidene)methyl)phenoxy)acetate
Parent CAS No.
[1202076-01-4]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| SKI II - SKI 2 | Axon 2782
CAS [312636-16-1]
MF C15H11ClN2OSMW 302.78
Purity:
99%
Soluble in DMSO
Description
SKI II is an orally bioavailable sphingosine kinase (SK or SphK) inhibitor (IC50 value of 0.5 µM) without competition at the ATP-binding site of SK. Moreover, SKI II showed no inhibition on a small panel of human protein kinases (ERK2 and PKC-α) and a lipid kinase (PI3K). SKI II inhibited cancer cell proliferation, induced apoptosis and inhibited tumor growth in mice.
KEYWORDS: SKI II | supplier | SphK inhibitor | SKI 2 | SKIII | SKI-II | SKI2 | SKI-2 | CAS [312636-16-1] | Sphingosine | SphK1 | SphK2 | Inhibitor | Enzymes | Apoptosis | | axonmedchem |
| K6PC-5 | Axon 2484
CAS [756875-51-1]
MF C19H37NO4MW 343.50
Purity:
98%
Soluble in DMSO
Description
Sphingosine kinase 1 (SphK1 or SK1) activator that increases sphingosine-1-phosphate (S1P) production, induces Akt phosphorylation in cultured osteoblasts, and protects them from Dex-induced apoptosis and necrosis. K6PC-5 acts to regulate both differentiation and proliferation of keratinocytes via [Ca2+]i responses through S1P production, which may represent a novel approach for treatment of skin disorders characterized by abnormal differentiation and proliferation, such as atopic dermatitis and psoriasis. Furthermore, a useful tool in animal or clinical studies for its antiglucocorticoids-associated osteonecrosis potential.
KEYWORDS: K6PC-5 | supplier | SphK1 activator | K6PC5 | CAS [756875-51-1] | Sphingosine | SphK | Activator | sphingosine-1-phosphate | S1P | apoptosis | necrosis | epidermal | differentiation | proliferation | keratinocytes | calcium signaling | dermatitis | psoriasis | | axonmedchem |
| SSR 69071 | Axon 1269
CAS [344930-95-6]
MF C27H32N4O7SMW 556.63
Purity:
99%
Soluble in DMSO and Ethanol
Description
A highly potent human leukocyte elastase (HLE) inhibitor (Ki value 0.02 nM)
References
Certificates
Categories
Extra info
Z Kapui et al. Biochemical and pharmacological characterization of SSR69071, a novel orally active elastase inhibitor. J. Pharmacol. Exp. Ther. 2003, 102, 44263.
JP Bidouard et al. SSR69071, an elastase inhibitor, reduces myocardial infarct size following ischemia–reperfusion injury. Eur. J. Pharmacol. 2003, 461, 49-52.
Certificate of Analysis
Material Safety Data Sheet
Immunology
Miscellaneous
Pain & Inflammation
EC 3.4.21.37
HNE
HLE inhibitor
Chemical name
2-(4-Isopropyl-6-methoxy-1,1,3-trioxo-1,3-dihydro-1lambda*6*-benzo[d]isothiazol-2-ylmethoxy)-9-(2-piperidin-1-yl-ethoxy)-pyrido[1,2-a]pyrimidin-4-one
Parent CAS No.
[344930-95-6]
Order
Size
Unit Price
Stock
10 mg
€145.00
In Stock | | axonmedchem |
| Tiplaxtinin - PAI 039 | Axon 1383
CAS [393105-53-8]
MF C24H16F3NO4MW 439.38
Purity:
99%
Soluble in DMSO
Description
Inhibitor of plasminogen activator inhibitor-1 (PAI-1).
KEYWORDS: Tiplaxtinin | supplier | PAI-1 inhibitor | PAI 039 | PAI039 | PAI-039 | CAS [393105-53-8] | Serpin | Plasminogen activator inhibitor-1 (PAI-1) | thrombosis | diabetes | | axonmedchem |
| Apixaban - BMS 562247-01 | Axon 1754
CAS [503612-47-3]
MF C25H25N5O4MW 459.50
Purity:
98%
Soluble in DMSO
Description
Direct factor Xa inhibitor; being investigated as an anticoagulant
References
Certificates
Categories
Extra info
CB Grange et al. Apixaban versus Warfarin in Patients with Atrial Fibrillation. N. Engl. J. Med. 2011, 365, 981-992.
JH Alexander et al. Apixaban with antiplatelet therapy after acute coronary syndrome. N. Engl. J. Med. 2011, 365(8), 699-708.
SJ Connolly et al. Apixaban in patients with atrial fibrillation. N. Engl. J. Med. 2011, 364(9), 806–817.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Factor Xa
EC 3.4.21.6
Factor Xa inhibitor
Chemical name
1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
Parent CAS No.
[503612-47-3]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| RP 001 hydrochloride | Axon 1947
CAS [N.A.]
MF C24H24N4O4.HClMW 468.93
Purity:
99%
Soluble in DMSO
Description
A picomolar short-acting sphingosine-1-phosphate 1 (S1P1) receptor selective agonist (EC50: 9 pM)
References
Certificates
Categories
Extra info
SM Cahalan et al. Actions of a picomolar short-acting S1P₁agonist in S1P₁-eGFP knock-in mice. Nat. Chem. Biol. 2011, 7(5), 254-256.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Apoptosis
Cardiovascular
Immunology
Miscellaneous
S1PR1
A13
A picomolar S1PR1 agonist
Chemical name
3-(4-(5-(3-cyano-4-isopropoxyphenyl)-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-ylamino)propanoic acid hydrochloride
Parent CAS No.
[1306761-53-4]
Order
Size
Unit Price
Stock
5 mg
€110.00
In Stock | | axonmedchem |
| JTE 013 | Axon 1866
CAS [383150-41-2]
MF C17H19Cl2N7OMW 408.29
Purity:
99%
Soluble in DMSO
Description
Potent and selective sphingosine-1-phosphate (S1P) receptor 2 (S1P2) antagonist (IC50: 17.6 nM).
Deleted CAS number [547756-93-4]
References
Certificates
Categories
Extra info
E Yokoo et al. Sphingosine 1-Phosphate Inhibits Migration of RBL-2H3 Cells via S1P2: Cross-Talk between Platelets and Mast Cells. J. Biochem. 2004, 135(6), 673-681.
T McQuiston et al. Role of sphingosine-1-phosphate (S1P) and S1P receptor 2 in the phagocytosis of Cryptococcus neoformans by alveolar macrophages. Microbiology 2011, 157(5), 1416-1427.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Apoptosis
Cardiovascular
Immunology
Miscellaneous
S1PR2
A13
S1PR2 antagonist
Chemical name
N-(2,6-dichloropyridin-4-yl)-2-(4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)hydrazinecarboxamide
Parent CAS No.
[383150-41-2]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| Mirabegron - YM 178 | Betanis | Axon 2414
CAS [223673-61-8]
MF C21H24N4O2SMW 396.51
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Highly selective and orally active agonist of the human β3-adrenoceptor (EC50 value 22.4 nM) with >440 fold selectivity over β1, and β2. FDA approved therapeutic drug for the treatment of symptoms of overactive bladder such as urinary frequency, urgency, and urge incontinence. YM178 (Mirabegron) does not affect the amplitude of rhythmic bladder contractions at doses at which it reduces contraction frequency.
References
Certificates
Categories
Extra info
T. Takasu et al. Effect of (R)-2-(2-aminothiazol-4-yl)-4'-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl} acetanilide (YM178), a novel selective beta3-adrenoceptor agonist, on bladder function. J Pharmacol Exp Ther. 2007 May;321(2):642-7.
E. Sacco et al. Mirabegron: a review of recent data and its prospects in the management of overactive bladder. Ther Adv Urol. 2012 Dec;4(6):315-24.
N. Aizawa et al. Effects of mirabegron, a novel β3-adrenoceptor agonist, on primary bladder afferent activity and bladder microcontractions in rats compared with the effects of oxybutynin. Eur Urol. 2012 Dec;62(6):1165-73.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
A17
Adrenoceptor β3
Highly selective and orally active agonist of the human β3-adrenoceptor
Chemical name
(R)-2-(2-aminothiazol-4-yl)-N-(4-(2-(2-hydroxy-2-phenylethylamino)ethyl)phenyl)acetamide
Parent CAS No.
[223673-61-8]
Order
Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |