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PF-915275

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Chemical Structure| 857290-04-1 同义名 : -
CAS号 : 857290-04-1
货号 : A271634
分子式 : C18H14N4O2S
纯度 : 99%+
分子量 : 350.394
MDL号 : MFCD12828758
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(85.62 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 PF-915275 stands out as a potent, selective, and orally active inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1), with a Ki of 2.3 nM and an EC50 of 15 nM in HEK293 cells. This inhibitor demonstrates a dose-dependent reduction in cortisone to cortisol conversion in primary human and monkey hepatocytes, with EC50 values of 20 nM and 100 nM, respectively[1].[2].[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.85mL

0.57mL

0.29mL

14.27mL

2.85mL

1.43mL

28.54mL

5.71mL

2.85mL
参考文献

[1]Bhat BG, et al. 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 11 -hydroxysteroid dehydrogenase type 1, in cynomolg

[2]Siu M, et al. N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3493-7.

[3]Courtney R, et al. Modulation of 11beta-hydroxysteroid dehydrogenase (11betaHSD) activity biomarkers and pharmacokinetics of PF-00915275, a selective 11betaHSD1 inhibitor. J Clin Endocrinol Metab. 2008 Feb;93(2):550-6.