857290-04-1
Chemical Structure
PF-915275
- CAS 番号: 857290-04-1
- Formula:C18H14N4O2S
- Molecular Weight:350.39
IUPAC Name: N-(6-aminopyridin-2-yl)-4'-cyano-[1,1'-biphenyl]-4-sulfonamide
InChIKey: ZESFDAKNYJQYKO-UHFFFAOYSA-N
SMILES: N#CC1=CC=C(C2=CC=C(S(NC3=NC(N)=CC=C3)(=O)=O)C=C2)C=C1
Biological Activity: PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively[1][2][3].
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PF-915275 | 98.59% | PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively. | ||||||||||||||||||||
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PF-915275 (Standard) | ≥98% | PF-915275 (Standard) is the analytical standard of PF-915275. This product is intended for research and analytical applications. PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively. | ||||||||||||||||||||
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- [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 cynomolgus monkeys. J Pharmacol Exp Ther. 2008 Jan;324(1):299-305. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
Keywords
