PF 915275

• Supplier: Tocris Bioscience
• Catalog: 4078
• Prices: $155.00, $645.00
• Sizes: 10 mg, 50 mg
• Function Type: Inhibitor
• Cas Number: 857290-04-1
• Chemical Name: N-(6-Amino-2-pyridinyl)-4'-cyano-[1,1'-biphenyl]-4-sulfonamide
• Formula: C18H14N4O2S
• Molecular Weight: 350.39
• Purity: >98 %
• Description: Potent and selective 11 β -hydroxysteroid dehydrogenase type 1 (11 β HSD1) inhibitor (K i = 2.3 nM) that displays little activity at 11 β HSD2 (1.5% inhibition at 10 μ M). Inhibits the conversion of prednisone to prednisolone in human hepatocytes in vitro (EC 50 = 15 nM) and has antidiabetic activity in vivo . Orally active.

Product References

Demonstration of proof of mechanism and pharmacokinetics and pharmacodynamic - Demonstration of proof of mechanism and pharmacokinetics and pharmacodynamic

Bhat BG, Hosea N, Fanjul A, Herrera J, Chapman J, Thalacker F, Stewart PM, Rejto PA. J Pharmacol Exp Ther. 2008 Jan;324(1):299-305. Epub 2007 Oct 5.

Modulation of 11beta-hydroxysteroid dehydrogenase (11betaHSD) activity biomarkers - Modulation of 11beta-hydroxysteroid dehydrogenase (11betaHSD) activity biomarkers

Courtney R, Stewart PM, Toh M, Ndongo MN, Calle RA, Hirshberg B. J Clin Endocrinol Metab. 2008 Feb;93(2):550-6. Epub 2007 Nov 6.

Blockade of glucocorticoid excess at the tissue level: inhibitors of - Blockade of glucocorticoid excess at the tissue level: inhibitors of

Fotsch C, Wang M. J Med Chem. 2008 Aug 28;51(16):4851-7.