| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| SEW 2871 | Axon 1672
CAS [256414-75-2]
MF C20H10F6N2OSMW 440.36
Purity:
100%
Soluble in DMSO
Description
Potent, cell-permeable and selective sphingosine-1-phosphate 1 (S1P1) receptor agonist (EC50: 13 nM); Does not activate S1P2, S1P3, S1P4 or S1P5 receptors at concentrations up to 10 μM
References
Certificates
Categories
Extra info
JJ Hale et al. A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists. J. Med. Chem. 2004, 47 6662.
MG Sanna et al. Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate. J. Biol. Chem. 2004, 279 13839.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Apoptosis
Cardiovascular
Immunology
Miscellaneous
S1PR1
A13
S1PR1 agonist
Chemical name
5-(4-phenyl-5-(trifluoromethyl)thiophen-2-yl)-3-(3-(trifluoromethyl)phenyl)-1,2,4-oxadiazole
Parent CAS No.
[256414-75-2]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| Sulfasalazine - SSZ | Axon 2070
CAS [599-79-1]
MF C18H14N4O5SMW 398.39
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
An old drug with new applications.
A Sulfa drug developed in 1950s and used in the treatment of inflammatory bowel disease and rheumatoid arthritis. This old drug was found in recent study to reverse severe liver disease. Sulfasalazine (SSZ) is a potent and selective inhibitor of NF-κB activation via its ability to block the activity of the inhibitor of κB (IκB) kinases α and β (IKKα and IKKβ). Sulfasalazine stimulates apoptosis of activated hepatic stellate cells and recovery from CCl4-induced fibrosis
References
Certificates
Categories
Extra info
F Oakley et al. Inhibition of inhibitor of κB kinases stimulates hepatic stellate cell apoptosis and accelerated recovery from rat liver fibrosis. Gastroenterology 2005, 128(1), 108–120.
C Wahl et al. Sulfasalazine: a potent and specific inhibitor of nuclear factor kappa B. J. Clin. Invest. 1998, 101(5), 1163.
CK Weber et al. Suppression of NF-kappaB activity by sulfasalazine is mediated by direct inhibition of IkappaB kinases alpha and beta. Gastroenterology. 2000, 119(5), 1209-1218.
S Liptay et al. Molecular mechanisms of sulfasalazine-induced T-cell apoptosis. Br. J. Pharmacol. 2002, 137(5), 608-620.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
Pain & Inflammation
Transcription Factors
NF-κB
EC 2.7.11.10
IKK
Pfizer Licensed Products
IKK inhibitor
Chemical name
2-hydroxy-5-((4-(N-pyridin-2-ylsulfamoyl)phenyl)diazenyl)benzoic acid
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[599-79-1]
Order
Size
Unit Price
Stock
25 mg
€45.00
In Stock | | axonmedchem |
| NS 19504 | Axon 2329
CAS [327062-46-4]
MF C10H9BrN2SMW 269.16
Purity:
99%
Soluble in DMSO
Description
Potent activator of large-conductance Ca2+-activated potassium channels (BK, KCa1.1, MaxiK; EC50 value 11 µM in a Tl+ assay) with a favorable selectivity profile in a screen of 68 receptors and by functional tests on Nav, Cav, SK, and IK channels. NS19504 potently inhibits urinary bladder spontaneous phasic contractions (SPCs) while having only a modest effect on contractions evoked by electrical field stimulation (EFS) and no effect on high K+-induced contractions. At a concentration of 10 µM, NS19504 was also found to inhbit the σ1 receptor, two transporters of neurotransmiters (DA and Norepinephrine), and soluble epoxide hydrolase (sEH).
References
Certificates
Categories
Extra info
B. Nausch et al. NS19504: a novel BK channel activator with relaxing effect on bladder smooth muscle spontaneous phasic contractions. J Pharmacol Exp Ther. 2014 Sep;350(3):520-30.
Y. Amano et al. Structural insights into binding of inhibitors to soluble epoxide hydrolase gained by fragment screening and X-ray crystallography. Bioorg Med Chem. 2014 Apr 15;22(8):2427-34.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
KCa1.1
DRI
NRI
KCNMA1
Potent activator of large-conductance Ca2+-activated potassium (BK) channels
Chemical name
5-(4-bromobenzyl)thiazol-2-amine
Parent CAS No.
[327062-46-4]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| CoPo 22 | Axon 1763
CAS [606101-83-1]
MF C22H22N4O2MW 374.44
Purity:
99%
Soluble in DMSO
Description
Corrector and potentiator (Co-Po) for ∆F508-cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel function in cystic fibrosis, with low micromolar EC50
References
Certificates
Categories
Extra info
PW Phuan et al. Cyanoquinolines with Independent Corrector and Potentiator Activities Restore ∆F508-CFTR Chloride Channel Function in Cystic Fibrosis. Mol. Pharmacol. 2011, 80(4), 683-693.
AS Verkman et al. CFTR chloride channel drug discovery--inhibitors as antidiarrheals and activators for therapy of cystic fibrosis. Curr. Pharm. Des. 2006; 12(18), 2235-2247.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CFTR
EC 3.6.3.49
Modulator of CFTR (δ-F508 Selective)
Chemical name
N-(2-(3-cyano-5,7-dimethylquinolin-2-ylamino)ethyl)-3-methoxybenzamide
Parent CAS No.
[606101-83-1]
Order
Size
Unit Price
Stock
5 mg
€120.00
In Stock | | axonmedchem |
| MIBG hemisulfate - Iobenguane hemisulfate | Axon 1750
CAS [87862-25-7]
MF C8H10IN3.0.5H2O4SMW 324.13
Purity:
99%
Soluble in DMSO
Description
MIBG standard; Radioiodinated iobenguane (or MIBG) is a radiopharmaceutical, used in a scintigraphy method called MIBG scan. Radioiodinated iobenguane is used to treat certain kinds of cancer of the adrenal glands.
KEYWORDS: MIBG hemisulfate | MIBG standard | Iobenguane hemisulfate | CAS [87862-25-7] | [80663-95-2] | [103346-16-3] | [80663-96-3] | Adrenaline, (Nor-) | Adrenoceptor α1 | Adrenoceptor α2 | Adrenoceptor β1 | Adrenoceptor β2 | Agonist | Receptors | | axonmedchem |
| NS 1619 | Axon 2854
CAS [153587-01-0]
MF C15H8F6N2O2MW 362.23
Purity:
98%
Soluble in DMSO
Description
NS 1619 is a selective large-conductance Ca2+-activated K+ channel (BK channel) activator which decreased the mitochondrial membrane potential with an EC50 value of 3.6 μM. Besides induction of apoptosis, NS 1619 inhibits both mitochondrial function in the glioma cell line LN229, as well as proliferation of A2780 cells (IC50 value of 31.1 μM). These anticancer activities are associated with increased expression of p53, p21, and Bax.
KEYWORDS: NS 1619 | supplier | BK channel activator | NS1619 | NS-1619 | CAS [153587-01-0] | Potassium | KCa1.1 | Opener | Ion Channels | Apoptosis | Glioma | A2780 | p53 | p21 | Bax | | axonmedchem |
| TAK 259 | Axon 2579
CAS [1192347-42-4]
MF C14H13Cl2N3O3S.HClMW 410.70
Purity:
99%
Soluble in water and DMSO
Description
Novel, selective, and orally active α1D adrenoceptor antagonist (Ki value 1.1 nM, and 200-800 fold selective over α1A and α1B, respectively) with anti-urinary frequency effects: reducing human Ether-a-go-go-Related Gene (hERG) liabilities. Clinical candidate, and a promising novel therapeutic agent for the treatment of OAB (overactive bladder) symptoms.
KEYWORDS: TAK 259 | supplier | α1D antagonist | TAK259 | CAS [1192347-42-4] | [1192348-73-4] | Adrenaline | Adrenoceptor α1 | GPCR | anti-urinary | hERG liabilities | human Ether-a-go-go-Related Gene | overactive bladder | OAB | | axonmedchem |
| IBP, 4- - NSC 667672 | Axon 2919
CAS [155798-08-6]
MF C19H21IN2OMW 420.29
Purity:
98%
Soluble in DMSO
Description
4-IBP is a selective sigma-1 (σ-1) agonist with Ki values of 1.70 nM and 25.2 nM for σ-1 and σ-2 receptor subtypes, respectively. Activating the σ-1 receptor with noncytotoxic doses of 4-IBP decreases the migration levels of various types of cancer cells, including C32 melanoma, U373-MG glioblastoma, A549 NSCLC, and PC3 prostate cancer cells. Moreover, 4-IBP sensitizes these cancer cells in vitro and in vivo to cytotoxic insults of proapoptotic and proautophagic drugs.
KEYWORDS: 4-IBP | supplier | Sigma-1 agonist | NSC 667672 | 4IBP | 4 IBP | NSC667672 | NSC-667672 | CAS [155798-08-6] | Sigma Receptor Substrates | Sigma-1 | Antagonist | Receptors | | axonmedchem |
| Modafinil - CRL 40476 | GRL 40476 | CN 801 | Axon 1296
CAS [68693-11-8]
MF C15H15NO2SMW 273.35
Purity:
99%
Soluble in DMSO and Ethanol
Description
α1 Adrenergic receptor agonist; psychoanaleptic agent with central nervous stimulant properties; a eugeroic drug generally prescribed to treat narcolepsy
References
Certificates
Categories
Extra info
A Besset et al. Use of modafinil in the treatment of narcolepsy: A long term follow-up study. Neurophysiol Clin. 1996, 26(1), 60-66.
PM Becker et al. Randomized trial of modafinil as a treatment for the excessive daytime somnolence in narcolepsy. Neurology 2000, 54(5), 1166-1175.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Adrenoceptor α1
A17
α1 adrenoceptor agonist
Chemical name
2-(Diphenyl-methanesulfinyl)-acetamide
Parent CAS No.
[68693-11-8]
Order
Size
Unit Price
Stock
10 mg
€55.00
In Stock | | axonmedchem |
| BD 1063 dihydrochloride | Axon 2088
CAS [206996-13-6 ]
MF C13H18Cl2N2.2HClMW 346.12
Purity:
100%
Soluble in water and DMSO
Description
Potent and selective sigma-1 (σ-1) receptor antagonist (Ki=9 nM); about 50-fold more selective for sigma-1 over sigma-2 and >100-fold more selective over 9 other tested neurotransmitter receptors; shown to antagonize cocaine efffects
References
Certificates
Categories
Extra info
V Sabino et al. The σ-Receptor Antagonist BD-1063 Decreases Ethanol Intake and Reinforcement in Animal Models of Excessive Drinking. Neuropsychopharmacology 34.6 (2008): 1482-1493.
KA McCracken et al. Novel σ receptor ligands attenuate the locomotor stimulatory effects of cocaine. Eur. J. Pharmacol. 1995, 365(1), 35-38.
FP Monnet et al. Neurosteroids, via sigma receptors, modulate the [3H] norepinephrine release evoked by N-methyl-D-aspartate in the rat hippocampus. Proc. Nat. Acad. Sci. 1995, 92(9), 3774-3778.
Certificate of Analysis
Material Safety Data Sheet
CNS
Sigma
Unclassified
Selective sigma-1 (σ-1) receptor antagonist
Chemical name
1-(3,4-dichlorophenethyl)-4-methylpiperazine dihydrochloride
Parent CAS No.
[150208-28-9]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| Prazosin hydrochloride - Furazosin hydrochloride | Axon 2040
CAS [19237-84-4]
MF C19H21N5O4.HClMW 419.86
Purity:
99%
Soluble in DMSO
Description
Peripherally acting α1 adrenergic receptor antagonist; an antihypertensive
References
Certificates
Categories
Extra info
D Cambridge et al. Prazosin, a selective antagonist of post-synaptic alpha-adrenoceptors [proceedings]. Br. J. Pharmacol. 1977, 59(3), 514P–515P.
J. Koch-Weser et al. Drug therapy. Prazosin. N. Engl. J. Med. 1979, 300(5), 232-236.
P Greengrass, R Bremmer. Binding characteristics of 3H-prazosin to rat brain α-adrenergic receptors. Eur. J. Pharmacol. 1979, 55(3), 323–326.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Adrenoceptor α1
A17
Pfizer Licensed Products
Peripherally acting α1 adrenoceptor antagonist
Chemical name
(4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl)(furan-2-yl)methanone hydrochloride
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[19216-56-9]
Order
Size
Unit Price
Stock
10 mg
€50.00
In Stock | | axonmedchem |
| SA 4503 - Cutamesine | Axon 1767
CAS [165377-44-6]
MF C23H32N2O2.2HClMW 441.43
Purity:
99%
Soluble in water
Description
Potent and selective sigma-1 receptor agonist; showing high affinity (IC50=17.4 nM) for sigma-1 and 100 fold less affinity for sigma-2.
KEYWORDS: SA 4503 | supplier | Sigma-1 antagonist | Cutamesine | SA4503 | SA-4503 | CAS [165377-44-6] | [165377-43-5] | Sigma Receptor Substrates | Sigma-1 | Antagonist | Receptors | | axonmedchem |
| AVE 0118 hydrochloride | Axon 2243
CAS [498577-53-0 (parent)]
MF C30H29N3O3.HClMW 516.03
Purity:
99%
Soluble in water and DMSO
Description
Potassium channel blocker. AVE0118 caused concentration-dependent inhibition of Kv1.5 (IKur), Kv4.3 (Ito), Kir3.4 (IKAch), and IKr currents (IC50 values 6.2 μM, 3.4 μM, 4.5 μM, and 10 μM resp.). A potent and atrium selective antiarrhythmic compound with no apparent effect on ventricular repolarization. Noteworthy, the atrial selective and dose-dependent prolongation of atrial refractoriness (ERP) by AVE 0118 has been claimed to be an inhibitory effect of sodium channel activity in an atrial-selective manner, and may therefor contribute to anti-AF properties of AVE0118.
References
Certificates
Categories
Extra info
H. Gögelein et al. Effects of the atrial antiarrhythmic drug AVE0118 on cardiac ion channels. Naun. Schmiedebergs Arch. Pharmacol. 2004, 370, 183-192.
K.J. Wirth et al. Atrial effects of the novel K+-channel-blocker AVE0118 in anesthetized pigs. Cardiovascular Res. 2003, 60, 298-306.
A. Burashnikov et al. Atrial-selective prolongation of refractory period with AVE0118 is due principally to inhibition of sodium channel activity. J. Cardiovasc. Pharmacol. 2012, 59, 539-546.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Pain & Inflammation
Kv1.5
Kv4.3
Kir4.3
KCND3
KCNJ5
KCNE1
Potassium channel blocker (Kv1.5 (IKur), Kv4.3 (Ito), Kir3.4 (IKAch), and IKr currents)
Chemical name
2'-((2-(4-methoxyphenyl)acetamido)methyl)-N-(2-(pyridin-3-yl)ethyl)biphenyl-2-carboxamide hydrochloride
Parent CAS No.
[498577-53-0]
Order
Size
Unit Price
Stock
5 mg
€120.00
In Stock | | axonmedchem |
| PB 28 dihydrochloride | Axon 1272
CAS [172907-03-8]
MF C24H38N2O.2HClMW 443.49
Purity:
99%
Soluble in water
Description
High affinity sigma-2 agonist
References
Certificates
Categories
Extra info
G Cassano et al. The sigma-2 receptor agonist PB28 inhibits calcium release from the endoplasmic reticulum of SK-N-SH neuroblastoma cells. Cell Calcium 2006, 40(1), 23-28.
A Azzariti et al. Cyclohexylpiperazine derivative PB28, a sigma2 agonist and sigma1 antagonist receptor, inhibits cell growth, modulates P-glycoprotein, and synergizes with anthracyclines in breast cancer. Mol. Cancer Ther. 2006, 5(7), 1807-1816.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Sigma
Unclassified
Sigma-2 agonist
Chemical name
1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydro-naphthalen-1-yl)-propyl]-piperazine dihydrochloride
Parent CAS No.
[172906-90-0]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| BD 1047 dihydrobromide | Axon 1215
CAS [138356-21-5]
MF C13H20Cl2N2.HBrMW 437.04
Purity:
99%
Soluble in water
Description
Sigma-1 receptor antagonist
References
Certificates
Categories
Extra info
G Skuza and Z Rogóz. Effect of BD 1047, a sigma1 receptor antagonist, in the animal models predictive of antipsychotic activity. Pharmacol Rep. 2006, 58(5), 626-35.
N. Egashira et al. Involvement of the sigma1 receptor in inhibiting activity of fluvoxamine on marble-burying behavior: Comparison with paroxetine. Eur. J. Pharmacol. 2007, 563(1-3), 149-154.
Certificate of Analysis
Material Safety Data Sheet
CNS
Sigma
Unclassified
Sigma-1 antagonist
Chemical name
N-[2-(3,4-Dichloro-phenyl)-ethyl]-N,N',N'-trimethyl-ethane-1,2-diamine dihydrobromide
Parent CAS No.
[138356-20-4]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| PK-THPP | Axon 2403
CAS [1332454-07-5]
MF C29H32N4O2MW 468.59
Purity:
99%
Soluble in DMSO
Description
Potent TASK-3 (KCNK9) antagonist (IC50 value 303 nM and 35nM for TASK-1 and TASK-3, respectively) with >140 fold selectivity over a wider range of potassium channels. PK-THPP produced a significant increase in active wake with a concurrent decrease in both REM and delta sleep immediately following administration to wild-type (WT) mice, and stimulated breathing by increasing tidal volume and breathing rate in isoflurane-anesthetized rats. PK-THPP induced a respiratory alkalosis and increased oxygenation.
References
Certificates
Categories
Extra info
D.P. Flaherty et al. Potent and selective inhibitors of the TASK-1 potassium channel through chemical optimization of a bis-amide scaffold. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3968-73.
C.A. Coburn et al. Discovery of a pharmacologically active antagonist of the two-pore-domain potassium channel K2P9.1 (TASK-3). ChemMedChem. 2012 Jan 2;7(1):123-33.
J.F. Cotten. TASK-1 (KCNK3) and TASK-3 (KCNK9) tandem pore potassium channel antagonists stimulate breathing in isoflurane-anesthetized rats. Anesth Analg. 2013 Apr;116(4):810-6.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
TASK-3
Potent TASK-3 antagonist with selectivity over a wide range of potassium channels
Chemical name
1-(1-(6-(Biphenylcarbonyl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl)piperidin-4-yl)butan-1-one
Parent CAS No.
[1332454-07-5]
Order
Size
Unit Price
Stock
10 mg
€145.00
In Stock | | axonmedchem |
| Retigabine dihydrochloride - D 23129 hydrochloride | Ezogabine dihydrochloride | Axon 2252
CAS [150812-13-8]
MF C16H18FN3O2.2HClMW 376.25
Purity:
99%
Soluble in water and DMSO
Description
Selective neuronal KCNQ/Kv7 potassium channel opener; an anticonvulsant in development for the potential oral treatment of complex partial seizures and post-herpetic neuralgia (PHN) The parent compound, Retigabine (Axon 1525), is available as well.
KEYWORDS: Retigabine HCl | supplier | KCNQ channel opener | D23129 HCl | Ezogabine HCl | D-23129 | CAS [150812-13-8] | [150812-12-7] | Potassium | Kv7.1 | neuronal | anticonvulsant | oral treatment | seizures | post-herpetic neuralgia | PHN | | axonmedchem |
| Dofetilide - UK 68798 | Axon 2103
CAS [115256-11-6]
MF C19H27N3O5S2MW 441.56
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent and selective potassium channel blocker, specific on subunit Kv11.1 (hERG) channel; selectively inhibits the rapid delayed-rectifier K+ current (IKr); a class III antiarrhythmic
References
Certificates
Categories
Extra info
M Gwilt et al. UK-68,798: a novel, potent and highly selective class III antiarrhythmic agent which blocks potassium channels in cardiac cells. J. Pharmacol. Expe. Ther. 1991, 256(1), 318-324.
C Torp-Pedersen et al. Dofetilide in patients with congestive heart failure and left ventricular dysfunction. N. Engl. J. Med. 1999, 341(12), 857-865.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Pain & Inflammation
Kv11.1
KCNH2
Pfizer Licensed Products
Kv11.1 (hERG) channel blocker
Chemical name
N-(4-(2-(methyl(2-(4-(methylsulfonamido)phenoxy)ethyl)amino)ethyl)phenyl)methanesulfonamide
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[115256-11-6]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| ML 335 | Axon 2872
CAS [825658-06-8]
MF C15H14Cl2N2O3SMW 373.25
Purity:
99%
Soluble in DMSO
Description
ML 335 is a selective K2P2.1 (TREK-1; KCNK2) and K2P10.1 (TREK-2; KCNK10) activator with EC50 values of 14.3 µM and 5.2 µM, respectively.
KEYWORDS: ML 335 | supplier | TREK activator | ML335 | ML-335 | CAS [825658-06-8] | Potassium | TREK | Activator | Ion Channels | TREK-1 | TREK-2 | K2P2.1 | K2P10.1 | KCNK2 | KCNK10 | | axonmedchem |
| ML 365 | Axon 2840
CAS [947914-18-3]
MF C22H20N2O3MW 360.41
Purity:
99%
Soluble in DMSO
Description
Potent and selective inhibitor of the TASK-1 (KCNK3) potassium channel (IC50 value of 4 nM) with 62-fold selectivity over TASK-3 in an orthogonal electrophysiology assay.
KEYWORDS: ML 365 | supplier | TASK-1 inhibitor | ML365 | ML-365 | CAS [947914-18-3] | Potassium | TASK-1 | Inhibitor | Ion Channels | KCNK3 | K2P3.1 | | axonmedchem |
| ICA-069673 | Axon 2724
CAS [582323-16-8]
MF C11H6ClF2N3OMW 269.63
Purity:
99%
Soluble in DMSO
Description
ICA-069673, a Kv7.2/Kv7.3 (KCNQ2/Q3) channel opener (EC50 value 0.69 μM), demonstrated 20-fold greater selectivity for heteromeric Kv7.2/Kv7.3 channels over Kv7.3/Kv7.5. Moreover, compared to retigabine (Axon 1525), ICA-069673 exhibits much stronger effects on KCNQ2 channels, including a large hyperpolarizing shift of the voltage-dependence of activation, an ~2-fold enhancement of peak current and pronounced subtype specificity for KCNQ2 over KCNQ3. Orally active in several animal models of epilepsy.
KEYWORDS: ICA-069673 | supplier | KCNQ channel opener | ICA069673 | ICA 069673 | CAS [582323-16-8] | Potassium | Kv7.2 | Kv7.3 | Opener | Ion Channels | KCNQ2 | KCNQ3 | Anti-convulsant | KCNQ2/Q3 | | axonmedchem |
| Glibenclamide potassium salt - Glyburide potassium salt | Axon 2064
CAS [23047-14-5]
MF C23H26ClK2N3O5SMW 570.18
Purity:
99%
Soluble in water and DMSO
Description
Antidiabetic; KATP channel blocker; the drug inhibits the sulfonylurea receptor 1 (SUR1), the regulatory subunit of the ATP-sensitive potassium channels (KATP) in pancreatic β cells
References
Certificates
Categories
Extra info
F Tomai et al. Ischemic preconditioning during coronary angioplasty is prevented by glibenclamide, a selective ATP-sensitive K+ channel blocker. Circulation 1994, 90(2), 700-705.
A Marble. Glibenclamide, a new sulphonylurea: whither oral hypoglycaemic agents? Drugs 1971, 1(2), 109–115.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
KCNJ11
Pfizer Licensed Products
Kir6.2-SUR1
KATP channel blocker; inhibits SUR1
Chemical name
5-chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide potassium
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[10238-21-8]
Order
Size
Unit Price
Stock
25 mg
€50.00
In Stock | | axonmedchem |
| NS 6180 | Axon 2094
CAS [353262-04-1]
MF C16H12F3NOSMW 323.33
Purity:
99%
Soluble in DMSO and Ethanol
Description
Potent KCa3.1 channel blocker with nanomolar potency
References
Certificates
Categories
Extra info
D Strøbæk et al. NS6180, a new K(Ca) 3.1 channel inhibitor prevents T-cell activation and inflammation in a rat model of inflammatory bowel disease. Br J Pharmacol. 2013, 168(2), 432-444.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Pain & Inflammation
KCa3.1
KCNN4
KCa3.1 channel blocker
Chemical name
4-(3-(trifluoromethyl)benzyl)-2H-benzo[b][1,4]thiazin-3(4H)-one
Parent CAS No.
[353262-04-1]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| Retigabine - D 23129 | Ezogabine | Axon 1525
CAS [150812-12-7]
MF C16H18FN3O2MW 303.33
Purity:
99%
Soluble in DMSO
Description
Selective neuronal KCNQ/Kv7 potassium channel opener; an anticonvulsant in development for the potential oral treatment of complex partial seizures and post-herpetic neuralgia (PHN) A water soluble form, Retigabine dihydrochloride (Axon 2252), is available as well.
KEYWORDS: Retigabine | supplier | KCNQ channel opener | D23129 | Ezogabine | Retigabine | D-23129 | CAS [150812-12-7] | Potassium | Kv7.1 | Ion Channel | neuronal | anticonvulsant | seizures | post-herpetic neuralgia | PHN | | axonmedchem |
| ML 297 - VU 0456810 | Axon 2436
CAS [1443246-62-5]
MF C17H14F2N4OMW 328.32
Purity:
99%
Soluble in DMSO
Description
First potent and selective activator of the GIRK potassium channel (EC50 value 0.16 µM for GIRK1/2 activation) with selectivity for GIRK1-containing GIRKs, exhibiting antiepileptic properties in vivo. ML297 showed equal or greater efficacy compared to a clinically active anti-seizure medication,sodium valproate, regardless of whether epilepsy was initiated chemically with PTZ or via electroshock.
References
Certificates
Categories
Extra info
K. Kaufmann et al. ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice. ACS Chem Neurosci. 2013 Sep 18;4(9):1278-86.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
GIRK
KCNJ3
First potent and selective activator of the GIRK potassium channel
Chemical name
1-(3,4-difluorophenyl)-3-(3-methyl-1-phenyl-1H-pyrazol-5-yl)urea
Parent CAS No.
[1443246-62-5]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| ML 213 - CID 3111211 | Axon 2747
CAS [489402-47-3]
MF C17H23NOMW 257.37
Purity:
99%
Soluble in DMSO
Description
ML 213 is a potent, selective, and brain penetrant KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) channel opener (EC50 values of 230 nM and 510 nM, respectively). Valuable tool compound for understanding KCNQ2 and KCNQ4 channels in regulating neuronal activity.
KEYWORDS: ML 213 | supplier | KCNQ channel opener | CID 3111211 | ML213 | ML-213 | CAS [489402-47-3] | Potassium | Kv7.2 | Kv7.4 | Opener | Ion Channels | KCNQ2 | KCNQ4 | | axonmedchem |
| HMR 1098 - HMR 1883 sodium salt | Axon 1757
CAS [261717-22-0]
MF C19H21ClN3NaO5S2MW 493.96
Purity:
98%
Soluble in water and DMSO
Description
KATP channel blocker; HMR 1098 acts by inactivating the ATP-sensitive potassium channels (KATP) responsible for potassium efflux. HMR 1098 is an inhibitor of Kir6.2/SUR1-composed K(ATP) channels
References
Certificates
Categories
Extra info
H Gögelein et al. Effects of the cardioselective KATP channel blocker HMR 1098 on cardiac function in isolated perfused working rat hearts and in anesthetized rats during ischemia and reperfusion. N. Schmiedebergs Arch Pharmacol. 2001, 364(1), 33-41.
HX ZHang et al. HMR 1098 is not an SUR isotype specific inhibitor of heterologous or sarcolemmal K ATP channels. J. Mol. Cell Cardiol. 2011, 50(3), 552-560.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
KCNJ11
Kir6.2-SUR1
K+ channel blocker (SUR1/Kir6.2 selective)
Chemical name
sodium (5-chloro-2-methoxybenzoyl)(4-methoxy-3-(N-(methylcarbamothioyl)sulfamoyl)phenethyl)amide
Parent CAS No.
[158751-64-5]
Order
Size
Unit Price
Stock
5 mg
€115.00
In Stock | | axonmedchem |
| Kv1.3 Channel blocker 42 | Axon 1735
CAS [N.A.]
MF C28H35FN2O4.HClMW 519.05
Purity:
99%
Soluble in water
Description
Potassium channel blocker, selective in blocking the Kv1.3 current (IC50: <50 nM); Selectivity: 25-fold over Kv1.1 and 24-fold over Kv1.5
References
Certificates
Categories
Extra info
AJ Harvey et al. Novel potassium channel blockers and uses thereof. Patent BIONOMICS LTD. WO2009149508 (A1)
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Immunology
Pain & Inflammation
Kv1.3
KCNA3
Kv1.3 potassium channel blocker
Chemical name
1-(7-(3-(4-fluorophenyl)butoxy)-2,4-dimethyl-6-(2-(piperidin-1-yl)ethoxy)benzo[d]oxazol-5-yl)ethanone Hydrochloride
Parent CAS No.
[1201582-43-5]
Order
Size
Unit Price
Stock
5 mg
€110.00
In Stock | | axonmedchem |
| S 9947 | Axon 1657
CAS [332378-43-5]
MF C29H27N3O3MW 465.54
Purity:
99%
Soluble in DMSO
Description
Kv1.5 or IKur channel blocker, which suppresses both cloned (Kv1.5) and native (IKur) cardiac potassium current
References
Certificates
Categories
Extra info
A Bachmann et al. Characterization of a novel Kv1.5 channel blocker in Xenopus oocytes, CHO cells, human and rat cardiomyocytes. Naunyn Schmiedebergs Arch Pharmacol. 2001, 364(5), 472-478.
K Knobloch et al. Electrophysiological and antiarrhythmic effects of the novel IKur channel blockers, S9947 and S20951, on left vs. right pig atrium in vivo in comparison with the IKr blockers (...). Naunyn-Schmiedebergs Arch. Pharmacol. 2002, 366, 482.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Pain & Inflammation
Kv1.5
KCNA5
Ikur/Kv1.5 channel Inhibitor
Chemical name
benzyl (2'-(2-(pyridin-2-yl)ethylcarbamoyl)biphenyl-2-yl)methylcarbamate
Parent CAS No.
[332378-43-5]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| Retigabine - D 23129 | Ezogabine | Axon 1525
CAS [150812-12-7]
MF C16H18FN3O2MW 303.33
Purity:
99%
Soluble in DMSO
Description
Selective neuronal KCNQ/Kv7 potassium channel opener; an anticonvulsant in development for the potential oral treatment of complex partial seizures and post-herpetic neuralgia (PHN) A water soluble form, Retigabine dihydrochloride (Axon 2252), is available as well.
KEYWORDS: Retigabine | supplier | KCNQ channel opener | D23129 | Ezogabine | Retigabine | D-23129 | CAS [150812-12-7] | Potassium | Kv7.1 | Ion Channel | neuronal | anticonvulsant | seizures | post-herpetic neuralgia | PHN | | axonmedchem |
| NN 414 - Tifenazoxide | Axon 1647
CAS [279215-43-9]
MF C9H10ClN3O2S2MW 291.78
Purity:
99%
Soluble in DMSO
Description
A potent and Kir6.2/SUR1 selective K(ATP) channels opener, which inhibits glucose stimulated insulin release in vitro and in vivo and has beneficial effects on glucose homeostasis in preclinical and clinical studies. Unfortunately, its clinical development was recently suspended due to elevated liver enzymes
References
Certificates
Categories
Extra info
RD Carr et al. NN414, a SUR1/Kir6.2-Selective Potassium Channel Opener, Reduces Blood Glucose and Improves Glucose Tolerance in the VDF Zucker Rat. Diabetes 2003, 52(10), 2513-2518.
M Zdravkovic et al. The effects of NN414, a SUR1/Kir6.2 selective potassium channel opener, in healthy male subjects. J. Clin. Pharmacol. 2005, 45(7), 763-772.
JB Hansen. Towards selective Kir6.2/SUR1 potassium channel openers, medicinal chemistry and therapeutic perspectives. Curr. Med. Chem. 2006, 13(4), 361-76.
M Zdravkovic et al. The effects of NN414, a SUR1/Kir6.2 selective potassium channel opener in subjects with type 2 diabetes. Exp. Clin. Endocrinol Diabetes. 2007, 115(6), 405-406.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Endocrinology
KCNJ11
Kir6.2-SUR1
K+ channel opener (SUR1/Kir6.2 selective)
Chemical name
6-Chloro-3-(1-methylcyclopropylamino)-4H-thieno[3,2-e][1,2,4]thiadiazine-1,1-dioxide
Parent CAS No.
[279215-43-9]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| EBIO, 1- | Axon 1313
CAS [10045-45-1]
MF C9H10N2OMW 162.19
Purity:
99%
Soluble in DMSO and Ethanol
Description
Ca2+-activated K+-channel opener
References
Certificates
Categories
Extra info
AS Adeagbo. 1-Ethyl-2-benzimidazolinone stimulates endothelial KCa channels and nitric oxide formation in rat mesenteric vessels. Eur. J. Pharmacol. 1999, 379, 151-159.
K.L. Hamilton, L. Meads and A.G. Butt. 1-EBIO stimulates Cl- secretion by activating a basolateral K+ channel in the mouse jejunum. Eur. J. Physiol. 1999, 439(1-2), 158-166.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
KCa1.1
KCNMA1
Stem Cell Differentiator
K+ channel opener (Ca2+ activated)
Chemical name
1-Ethyl-1,3-dihydro-benzoimidazol-2-one
Parent CAS No.
[10045-45-1]
Order
Size
Unit Price
Stock
10 mg
€50.00
In Stock | | axonmedchem |
| BMS 204352, (R)-(-)- | Axon 1309
CAS [187523-36-0]
MF C16H10ClF4NO2MW 359.70
Purity:
98%
Optical purity:
>98% ee
Soluble in DMSO
Description
Less active opposite R-(-)-enantiomer of S-(+)-enantiomer, BMS-204352 (Flindokalner, Axon 1112), a Maxi-K channel opener
References
Certificates
Categories
Extra info
Krishna R et al. Pharmacokinetics and dose proportionality of BMS-204352 after intraarterial administration to rats. Biopharm Drug Dispos. 2002, 23(6), 233-7.
M. P. G. Korsgaard et al. Anxiolytic Effects of Maxipost (BMS-204352) and Retigabine via Activation of Neuronal Kv7 Channels. J. Pharmacol. Exp. Ther. 2005, 314, 282-292.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
KCa1.1
KCNMA1
Potassium channel opener; Less active enantiomer of Axon 1112
Chemical name
(R)-3-(5-Chloro-2-methoxy-phenyl)-3-fluoro-6-trifluoromethyl-1,3-dihydro-indol-2-one
Parent CAS No.
[187523-36-0]
Order
Size
Unit Price
Stock
5 mg
€145.00
In Stock | | axonmedchem |
| DMP 543 | Axon 1322
CAS [160588-45-4]
MF C26H18F2N2OMW 412.43
Purity:
99%
Soluble in DMSO
Description
Neurotransmitter release enhancer, K+ channel blocker and acetylcholine release stimulator; potential AD therapeutic
References
Certificates
Categories
Extra info
Zaczek et al. Two new potent neurotransmitter release enhancers, 10,10-Bis(4-pyridinylmethyl)-9(10H)-anthracenone and 10,10-Bis(2-flouro-4-pyridinylmethyl) -9(10H)-anthracenone: comparison to linopirdine. J. Pharmacol. Exp. Ther. 1998, 285, 724.
Chorvat et al. Ion channel modulator that enhance acetylcholine release: potential therapies for Alzheimer's disease. Exp. Opin. Invest. Drugs. 1998, 7(4), 499-518.
Camps et al. Cholinergic Drugs in Pharmacotherapy of Alzheimer's Disease. Mini Rev. Med. Chem, 2002, 2, 11-25.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Pain & Inflammation
Non Selective
Unclassified
K+ channel blocker; Ach release stimulator
Chemical name
10,10-Bis-(2-fluoro-pyridin-4-ylmethyl)-10H-anthracen-9-one
Parent CAS No.
[160588-45-4]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| BMS 204352, (±)- | Axon 1308
CAS [183720-28-7]
MF C16H10ClF4NO2MW 359.70
Purity:
98%
Soluble in DMSO
Description
Potassium channel opener; racemate of more active S-(+)-enantiomer, BMS-204352 (Flindokalner, Axon 1112), and less active R-(-)-enantiomer (Axon 1309)
References
Certificates
Categories
Extra info
Krishna R et al. Pharmacokinetics and dose proportionality of BMS-204352 after intraarterial administration to rats. Biopharm Drug Dispos. 2002, 23(6), 233-7.
M. P. G. Korsgaard et al. Anxiolytic Effects of Maxipost (BMS-204352) and Retigabine via Activation of Neuronal Kv7 Channels. J. Pharmacol. Exp. Ther. 2005, 314, 282-292.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
KCa1.1
KCNMA1
Potassium channel opener; racemate of Axon 1112
Chemical name
3-(5-Chloro-2-methoxy-phenyl)-3-fluoro-6-trifluoromethyl-1,3-dihydro-indol-2-one
Parent CAS No.
[183720-28-7]
Inquire | | axonmedchem |
| Chromanol 293B | Axon 1294
CAS [163163-23-3]
MF C15H20N2O4SMW 324.40
Purity:
99%
Soluble in DMSO
Description
Blocker of the slow delayed rectifier K+ current via KCNQ1 channels
References
Certificates
Categories
Extra info
C Lengyel et al. Pharmacological block of the slow component of the outward delayed rectifier current (I(Ks)) fails to lengthen rabbit ventricular muscle QT(c) and action potential duration. Br. J. Pharmacol. 2001, 132, 101-110.
G Seebohm et al. A kinetic study on the stereospecific inhibition of KCNQ1 and I(Ks) by the chromanol 293B. Br. J. Pharmacol. 2001, 134, 1647-1654.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Pain & Inflammation
Kv7.1
KCNQ1
KCNQ1 channel blocker
Chemical name
Ethanesulfonic acid ((3R,4S)-6-cyano-3-hydroxy-2,2-dimethyl-chroman-4-yl)-methyl-amide (relative stereochemistry)
Parent CAS No.
[163163-23-3]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| XE 991 dihydrochloride | Axon 1305
CAS [122955-13-9]
MF C26H20N2O.2HClMW 449.37
Purity:
99%
Soluble in DMSO
Description
KCNQ channel and M-current blocker; potential AD therapeutic.The parent molecule of XE 991 (Axon 1987) is available as well.
References
Certificates
Categories
Extra info
Wang et al. KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel. Science 1998, 282 1890.
Zaczek et al. Two new potent neurotransmitter release enhancers, 10,10-bis(4-pyridinylmethyl)-9(10H)-anthracenone and 10,10-bis(2-fluoro-4-pyridinylmethyl) -9(10H)-anthracenone: comparison to linopirdine. J. Pharmacol. Exp. Ther. 1998, 285 724.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Pain & Inflammation
Kv7.1
KCNQ1
KCNQ channel and M-current blocker
Chemical name
10,10-bis(pyridin-4-ylmethyl)anthracen-9(10H)-one dihydrochloride
Parent CAS No.
[122955-42-4]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| BMS 204352 - Flindokalner | BMS 204352, (S)-(+)- | MaxiPost | Axon 1112
CAS [187523-35-9]
MF C16H10ClF4NO2MW 359.70
Purity:
99%
Optical purity:
99% ee
Soluble in DMSO
Description
Maxi-K channel opener, potential therapeutic for the treatment of stroke; more active S-(+)-enantiomer in comparison with R-(-)-enantiomer (Axon 1309)
References
Certificates
Categories
Extra info
R Krishna et al. Pharmacokinetics and dose proportionality of BMS-204352 after intraarterial administration to rats. Biopharm. Drug Dispos. 2002, 23(6), 233-7.
MPG Korsgaard et al. Anxiolytic Effects of Maxipost (BMS-204352) and Retigabine via Activation of Neuronal Kv7 Channels. J. Pharmacol. Exp. Ther.2005, 314, 282-292.
YK Son et al. The inhibitory effect of Ca2+-activated K+ channel activator, BMS on L-type Ca2+ channels in rat ventricular myocytes. Life sciences, 2011, 89(9), 331-336. (*BMS204352 used in this study is procured from Axon Medchem.)
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
KCa1.1
KCNMA1
Maxi K+ channel opener
Chemical name
(S)-3-(5-Chloro-2-methoxy-phenyl)-3-fluoro-6-trifluoromethyl-1,3-dihydro-indol-2-one
Parent CAS No.
[187523-35-9]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| Zatebradine hydrochloride - UL-FS 49 | Axon 1248
CAS [91940-87-3]
MF C26H36N2O5.HClMW 493.04
Purity:
99%
Soluble in water and DMSO
Description
HCN channel blocker: blocker of neuronal Ih, related cardiac If channels and ATP-sensitive Kir channels; specific bradycardic agent
References
Certificates
Categories
Extra info
PP Van Bogaert and F Pittoors. Use-dependent blockade of cardiac pacemaker current (If) by cilobradine and zatebradine. Eur. J. Pharmacol. 2003, 478, 161-171.
L Sen et al. Acute effects of zatebradine on cardiac conduction and repolarization. J. Cardiovasc. Pharmacol. 2002,7, 29-38.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
Pain & Inflammation
HCN
Unclassified
HCN channel blocker
Chemical name
3-(3-{[2-(3,4-Dimethoxy-phenyl)-ethyl]-methyl-amino}-propyl)-7,8-dimethoxy-1,3,4,5-tetrahydro-benzo[d]azepin-2-one hydrochloride
Parent CAS No.
[85175-67-3]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| Brimonidine tartrate - Alphagan-P | Axon 1555
CAS [70359-46-5]
MF C11H10BrN5.C4H6O6MW 442.22
Purity:
99%
Soluble in water and DMSO
Description
Selective α2-adrenergic receptor agonist, a drug used to treat open-angle glaucoma or ocular hypertension
References
Certificates
Categories
Extra info
C Toris et al. Acute versus chronic effects of brimonidine on aqueous humor dynamics in ocular hypertensive patients. Am. J. Ophthalmol. 1999, 128(1), 8–14.
Certificate of Analysis
Material Safety Data Sheet
CNS
Adrenoceptor α2
A17
α2 adrenoceptor agonist
Chemical name
5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl) quinoxalin-6-amine tartrate
Parent CAS No.
[59803-98-4]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| Atipamezole hydrochloride - Antisedan | MPV 1248 | Axon 1371
CAS [104075-48-1]
MF C14H16N2.HClMW 248.75
Purity:
99%
Soluble in water
Description
A competitive α2-adrenergic antagonist; used to antagonize (reverse) the action of the α2 adrenoceptor agonists medetomidine, xylazine and detomidine
References
Certificates
Categories
Extra info
R Virtanen et al. Highly selective and specific antagonism of central and peripheral alpha 2-adrenoceptors by atipamezole. Arch. Int. Pharmacodyn. Ther. 1989, 297 190-204.
K Puurunen et al. An α2-adrenergic antagonist, atipamezole, facilitates behavioral recovery after focal cerebral ischemia in rats. Neuropharmacol. 2001, 40, 597-606.
CW Jurgens et al. Alpha2A adrenergic receptor activation inhibits epileptiform activity in the rat hippocampal CA3 region. Mol Pharmacol. 2007, 71(6), 1572-1581.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Pain & Inflammation
Adrenoceptor α2
A17
α2 adrenoceptor antagonist
Chemical name
5-(2-Ethyl-indan-2-yl)-1H-imidazole hydrochloride
Parent CAS No.
[104054-27-5]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| ST 91 | Axon 1290
CAS [4749-61-5]
MF C13H19N3.HClMW 253.77
Purity:
99%
Soluble in water, DMSO and Ethanol
Description
α2 Adrenoceptor agonist
References
Certificates
Categories
Extra info
LS Stone et al. ST91-mediated spinal antinociception and synergy with opioids persists in the absence of functional alpha-2A- or alpha-2C-adrenergic receptors. J. Pharmacol. Exp. Ther. 2007, 323(3), 899-906.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Pain & Inflammation
Adrenoceptor α2
A17
α2 adrenoceptor agonist
Chemical name
(2,6-Diethyl-phenyl)-(4,5-dihydro-1H-imidazol-2-yl)-amine hydrochloride
Parent CAS No.
[4751-48-8]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| Celiprolol hydrochloride | Axon 1159
CAS [57470-78-7]
MF C20H33N3O4.HClMW 415.95
Purity:
98%
Soluble in water and DMSO
Description
A ß-blocker possessing strong ß1-adrenoceptor antagonist and mild ß2-agonist properties
References
Certificates
Categories
Extra info
Y Liao et al. Celiprolol, A Vasodilatory ß-Blocker, Inhibits Pressure Overload–Induced Cardiac Hypertrophy and Prevents the Transition to Heart Failure via Nitric Oxide–Dependent Mechanisms in Mice. Circulation. 2004, 110, 692-699.
FS Caruso et al. Effect of celiprolol, a new beta 1-alpha 2 blocker, on the cardiovascular response to exercise. J. Clin. Pharmacol. 1986; 26, 32-38.
M Cazzola et al. Comparison of the Effects of Single Oral Doses of Nebivolol and Celiprolol on Airways in Patients With Mild Asthma. Chest. 2000, 118, 1322-1326.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Adrenoceptor β1
A17
β1 antagonist
Chemical name
3-[3-Acetyl-4-(3-tert-butylamino-2-hydroxy-propoxy)-phenyl]-1,1-diethyl-urea hydrochloride
Parent CAS No.
[56980-93-9]
Order
Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| Bromobuterol | Axon 1157
CAS [41937-02-4]
MF C12H18Br2N2OMW 366.09
Purity:
98%
Soluble in DMSO and Ethanol
Description
β2 agonist
References
Certificates
Categories
Extra info
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Adrenoceptor β2
A17
β2 agonist
Chemical name
1-(4-Amino-3,5-dibromo-phenyl)-2-tert-butylamino-ethanol
Parent CAS No.
[41937-02-4]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| Efaroxan hydrochloride | Axon 1155
CAS [89197-00-2]
MF C13H16N2O.HClMW 252.74
Purity:
99%
Soluble in water and DMSO
Description
Selective α2-adrenoceptor antagonist
References
Certificates
Categories
Extra info
Mayer et al. Effects of the imidazoline ligands efaroxan and KU14R on blood glucose in the mouse. Eur. J. Pharmacol. 2002, 454, 95.
Certificate of Analysis
Material Safety Data Sheet
CNS
Adrenoceptor α2
A17
α2 adrenoceptor antagonist
Chemical name
2-(2-Ethyl-2,3-dihydro-benzofuran-2-yl)-4,5-dihydro-1H-imidazole hydrochloride
Parent CAS No.
[89197-32-0]
Order
Size
Unit Price
Stock
10 mg
€65.00
In Stock | | axonmedchem |
| B-HT 933 dihydrochloride - Azepexole | Axon 1154
CAS [36067-72-8]
MF C9H15N3O.2HClMW 254.16
Purity:
98%
Soluble in water and DMSO
Description
Selective α2-adrenoceptor agonist.
KEYWORDS: B-HT 933 dihydrochloride | supplier | α2 agonist | Azepexole | BHT933 HCl | CAS [36067-72-8] | [36067-73-9] | Adrenaline | Adrenoceptor alpha2 | GPCR | CNS | hypertension | arteries | contraction | | axonmedchem |
| SCH 79797 dihydrochloride | Axon 1275
CAS [1216720-69-2]
MF C23H25N5.2HClMW 444.40
Purity:
99%
Soluble in DMSO and Ethanol
Description
Potent and selective non-peptide PAR1 antagonist.
KEYWORDS: SCH 79797 dihydrochloride | supplier | PAR1 antagonist | SCH79797 HCl | CAS [1216720-69-2] | [245520-69-8] | Thrombin | PAR | myocardial | ischemia | reperfusion | GPCR | protease-activated receptor 1 | apoptosis | airway | inflammation | fibrosis | | axonmedchem |
| Ascorbyl octanoate, L- | Axon 1316
CAS [16690-38-3]
MF C14H22O7MW 302.32
Purity:
99%
Optical purity:
>98% ee
No solubility data
Description
Fat-soluble Vitamin C ester; antioxidant
References
Certificates
Categories
Extra info
Certificate of Analysis
Material Safety Data Sheet
Immunology
Miscellaneous
Antioxidant
Vitamin C ester; Antioxidant
Chemical name
Octanoic acid (S)-2-((R)-3,4-dihydroxy-5-oxo-2,5-dihydro-furan-2-yl)-2-hydroxy-ethyl ester
Parent CAS No.
[16690-38-3]
Order
Size
Unit Price
Stock
25 mg
€85.00
In Stock | | axonmedchem |
| AC 264613 | Axon 2898
CAS [1051487-82-1]
MF C19H18BrN3O2MW 400.27
Purity:
98%
Soluble in DMSO
Recently added | | axonmedchem |
| Q94 hydrochloride | Axon 2055
CAS [1052076-77-3]
MF C21H17ClN2.HClMW 369.29
Purity:
99%
Soluble in DMSO
Description
PAR1/Gαq-specific allosteric inhibitor or negative allosteric modulator (NAM); Q94 selectively blocks PAR1/Gαq interaction and signalling
References
Certificates
Categories
Extra info
X Ding et al. Thrombin induces fibroblast CCL2/JE production and release via coupling of PAR1 to Gαq and cooperation between ERK1/2 and Rho kinase signaling pathways. Mol. Biol. Cell, 2008, 19(6), 2520-2533.
S Asteriti et al. Modulation of PAR1 signalling by benzimidazole compounds. Br. J. Pharmacol. 2012, 167, 80–94.
PF Mercer et al. Pulmonary Epithelium Is a Prominent Source of Proteinase-activated Receptor-1–inducible CCL2 in Pulmonary Fibrosis. Am. J. Resp. Critical Care Med. 2009, 179(5), 414-425.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
A15
Thrombin (PAR)
Negative allosteric modulator of PAR1 (Gαq linkage)
Chemical name
2-benzyl-1-(4-chlorobenzyl)-1H-benzo[d]imidazole hydrochloride
Parent CAS No.
[537009-12-4]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |