PF-915275

• UNSPSC Description:

  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].

• Target Antigen:

  Others

• Type:

  Reference compound

• Related Pathways:

  Others

• Applications:

  Metabolism-sugar/lipid metabolism

• Field of Research:

  Metabolic Disease

• Assay Protocol:

  https://www.medchemexpress.com/PF-915275.html

• Solubility:

  DMSO : ≥ 31 mg/mL

• Smiles:

  N#CC1=CC=C(C2=CC=C(S(NC3=NC(N)=CC=C3)(=O)=O)C=C2)C=C1

• Molecular Weight:

  350.39

• References & Citations:

  [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.|[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.

• Shipping Conditions:

  Room Temperature

• Clinical Information:

  Phase 1

• CAS Number:

  857290-04-1