Chemical Name: N-(6-Amino-2-pyridinyl)-4'-cyano-[1,1'-biphenyl]-4-sulfonamide
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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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.
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
Modulation of 11β-hydroxysteroid dehydrogenase (11βHSD) activity biomarkers and pharmacokinetics of PF-00915275, a selective 11βHSD1 inhibitor.
Courtney et al.
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
Local cortisol activation is involved in EGF-induced immunosuppression.
Authors: Matsumura Et al.
An inhibitor of 11-β hydroxysteroid dehydrogenase type 1 (PF915275) alleviates nonylphenol-induced hyperadrenalism and adiposity in rat and human cells.
BMC Pharmacol Toxicol 2018;19(1):45
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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