PF 915275
Chemical Name: N-(6-Amino-2-pyridinyl)-4'-cyano-[1,1'-biphenyl]-4-sulfonamide
Purity: ≥98%
Biological Activity
PF 915275 is a potent 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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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 monke
Bhat et al.
J.Pharmacol.Exp.Ther., 2008;324:299 -
Blockade of glucocorticoid excess at the tissue level: inhibitors of 11β-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes.
Fotsch and Wang
J.Med.Chem., 2008;51:4851 -
Modulation of 11β-hydroxysteroid dehydrogenase (11βHSD) activity biomarkers and pharmacokinetics of PF-00915275, a selective 11βHSD1 inhibitor.
Courtney et al.
J.Clin.Endocrinol.Metab., 2008;93:550
Product Datasheets
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Citations for PF 915275
The citations listed below are publications that use Tocris products. Selected citations for PF 915275 include:
3 Citations: Showing 1 - 3
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Local cortisol activation is involved in EGF-induced immunosuppression.
Authors: Matsumura Et al.
Dermatoendocrinol 2018;9:e1412018
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An inhibitor of 11-β hydroxysteroid dehydrogenase type 1 (PF915275) alleviates nonylphenol-induced hyperadrenalism and adiposity in rat and human cells.
Authors: Chang
BMC Pharmacol Toxicol 2018;19(1):45
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Local blockade of glucocorticoid activation reverses stress- and glucocorticoid-induced delays in cutaneous wound healing.
Authors: Youm Et al.
Wound Repair Regen 2013;21:715
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