N-(6-Amino-2-pyridinyl)-4'-cyano-[1,1'-biphenyl]-4-sulfonamide

Biological Activity

PF-915275 is an orally active, potent and selective 11beta-hydroxysteroid dehydrogenase type 1 (11?-HSD1, HSD11B1) inhibitor (human 11?-HSD1 Ki <1 nM; cellular IC50 = 5 nM using human 11?-HSD1-transfected HEK293) with reduced potency toward non-human species (human/monkey/dog hepatocytes EC50 = 20/100/120 nM; mouse 11?-HSD1 Ki = 750 nM, r at hepatoma EC50 = 14 μM). PF-915275 (0.1-3-mg/kg via nasogastric intubations) inhibits prednisone-to-prednisolone conversion in cynomolgus monkeys (by 87% with 3 mg/kg) in vivo and reduces plasma insulin increase following prednisone & resumed feeding (4 hrs post PF-915275) among overnight fasted monkeys.

storage

Store at RT