| 产品名称 | ZK 216348, (+)- |
| 产品货号 | Axon 2239 CAS [669073-68-1] MF C24H23F3N2O5MW 476.45 Purity: 99% Optical purity: Optically pure Soluble in DMSO Description Selective nonsteroidal glucocorticoid receptor (GR) agonist for the treatment of experimental colitis with IC50 values of 20, 20, and 80 nM for GR, Progesterone (PR) and Mineralocorticoid (MR) receptors respectively. (+)-ZK 216348 shows antiinflammatory activity comparable to prednisolone for both systemic and topical application, with a significant dissociation between transrepression and transactivation of antiinflammatory effects both in vitro and in vivo.(+)-ZK 216348 showed no negative effects on intestinal epithelial migration or proliferation. (-)-ZK 216348 is completely inactive (IC50 >1000 nM for GR, PR, and MR. References Certificates Categories Extra info S. Jaroch te al. Discovery of quinolines as selective glucocorticoid receptor agonists. Bioorg. Med. Chem. Lett. 2010, 20, 5835-5838. H .Schäcke et al. Dissociation of transactivation from transrepression by a selective glucocorticoid receptor agonist leads to separation of therapeutic effects from side effects. Proc. Natl. Acad. Sci. USA. 2004, 101, 227-232. K.C. Reuter et al. Selective glucocorticoid receptor agonists for the treatment of inflammatory bowel disease: studies in mice with acute trinitrobenzene sulfonic acid colitis. J. Pharmacol. Exp. Ther. 2012, 341, 68-80. Certificate of Analysis Material Safety Data Sheet Cell Signaling & Oncology Immunology Pain & Inflammation Endocrinology NR3C Glucocorticoid (GR) Selective nonsteroidal glucocorticoid receptor (GR) agonist Chemical name (+)-4-(2,3-dihydrobenzofuran-7-yl)-2-hydroxy-4-methyl-N-(4-methyl-1-oxo-1H-benzo[d][1,2]oxazin-6-yl)-2-(trifluoromethyl)pentanamide Parent CAS No. [669073-68-1] Order Size Unit Price Stock 2 mg €125.00 In Stock |
| 产品价格 | 现货询价，电话：010-67529703 |
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| 产品品牌 | axonmedchem |
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| 产品详情 |
ZK 216348, (+)-Axon 2239 CAS [669073-68-1] MF C24H23F3N2O5
Description
Selective nonsteroidal glucocorticoid receptor (GR) agonist for the treatment of experimental colitis with IC50 values of 20, 20, and 80 nM for GR, Progesterone (PR) and Mineralocorticoid (MR) receptors respectively. (+)-ZK 216348 shows antiinflammatory activity comparable to prednisolone for both systemic and topical application, with a significant dissociation between transrepression and transactivation of antiinflammatory effects both in vitro and in vivo.(+)-ZK 216348 showed no negative effects on intestinal epithelial migration or proliferation. (-)-ZK 216348 is completely inactive (IC50 >1000 nM for GR, PR, and MR.
Selective nonsteroidal glucocorticoid receptor (GR) agonist
Chemical name(+)-4-(2,3-dihydrobenzofuran-7-yl)-2-hydroxy-4-methyl-N-(4-methyl-1-oxo-1H-benzo[d][1,2]oxazin-6-yl)-2-(trifluoromethyl)pentanamide Parent CAS No.[669073-68-1] |
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