Potent and selective 11β
-hydroxysteroid dehydrogenase type 1 (11β
HSD1) inhibitor (Ki
= 2.3 nM) that displays little activity at 11β
HSD2 (1.5% inhibition at 10 μ
M). Inhibits the conversion of prednisone to prednisolone in human hepatocytes in vitro
= 15 nM) and has antidiabetic activity in vivo
. Orally active.
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All Tocris products are intended for laboratory research use only.
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.