Cat. No. 3291
Chemical Name: N-(6-Amino-2-pyridinyl)-4'-cyano-[1,
Biological ActivityPotent and selective 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor (Ki = 2.3 nM) that displays little activity at 11βHSD2 (1.5% inhibition at 10 μM). Inhibits the conversion of prednisone to prednisolone in human hepatocytes in vitro (EC50 = 15 nM) and has antidiabetic activity in vivo. Orally active.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Safety Data Sheet
Bhat et al (2008) 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 11β-hydroxysteroid dehydrogenase type 1 in cynomolgus monkeys. J.Pharmacol.Exp.Ther. 324 299. PMID: 17921190.
Courtney et al (2008) Modulation of 11β-hydroxysteroid dehydrogenase (11βHSD) activity biomarkers and pharmacokinetics of PF-00915275, a selective 11βHSD1 inhibitor. J.Clin.Endocrinol.Metab. 93 550. PMID: 17986636.
Fotsch and Wang (2008) Blockade of glucocorticoid excess at the tissue level: inhibitors of 11β-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes. J.Med.Chem. 51 4851. PMID: 18652443.
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Keywords: PF 915275, supplier, Potent, selective, 11β-hydroxysteroid, beta-hydroxysteroid, dehydrogenases, type, 1, 11βHSD1, 11betaHSD1, inhibitors, inhibits, PF915275, Tocris Bioscience, 11β-Hydroxysteroid Dehydrogenase Inhibitor products
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