PF-915275
Product Specifications
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
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-18056/PF-915275-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-18056/PF-915275-SDS-MedChemExpress.pdf
Clinical Information
Phase 1
CAS Number
857290-04-1
Available Sizes
Curated Selection
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