| 货号 | 3291/50 |
| 别名 | N-(6-Amino-2-pyridinyl)-4'-cyano-[1, |
| 供应商 | Tocris |
| 生物活性 | Potent and selective 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor (Ki = 2.3 nM) that displays little activity at 11βHSD2 (1.5% inhibition at 10 μM). Inhibits the conversion of prednisone to prednisolone in human hepatocytes in vitro(EC50 = 15 nM) and has antidiabetic activity in vivo. Orally active. |
| 运输条件 | Blue Ice |
| 存放说明 | Ambient |
| 纯度 | >98 % |
| 计算分子量 | 350.39 |
| 分子式 | C18H14N4O2S |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO |
| CAS号 | 857290-04-1 |
| 参考文献 | Bhatet al (2008) Demonstration of proof of mechanism and pharmacokinetics and pharmacodynamic relationship with 4'-cyano-biphenyl-4-sulfonic acid (6-amino-pyridin-2-yl)-amide (PF-915275), an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 in cynomolgus monkeys. J.Pharmacol.Exp.Ther. 324 299. PMID: 17921190. Courtneyet al (2008) Modulation of 11β-hydroxysteroid dehydrogenase (11βHSD) activity biomarkers and pharmacokinetics of PF-00915275, a selective 11βHSD1 inhibitor. J.Clin.Endocrinol.Metab. 93 550. PMID: 17986636. Fotsch and Wang (2008) Blockade of glucocorticoid excess at the tissue level: inhibitors of 11β-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes. J.Med.Chem. 51 4851. PMID: 18652443. |