PF-915275 (C005B-432405)

Biochem/physiol Actions

PF-915275 is an orally active, potent and selective 11beta-hydroxysteroid dehydrogenase type 1 (11Ÿ-HSD1, HSD11B1) inhibitor (human 11Ÿ-HSD1 Ki <1 nM; cellular IC₅₀ = 5 nM using human 11Ÿ-HSD1-transfected HEK293) with reduced potency toward non-human species (human/monkey/dog hepatocytes EC₅₀ = 20/100/120 nM; mouse 11Ÿ-HSD1 Ki = 750 nM, rat 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.

Legal Information

Sold for research purposes under agreement from Pfizer Inc.

Orders outside of US, please allow an additional 1-2 weeks for delivery.

UPC:

51422101

Condition:

New

Weight:

1.00 Ounces

HazmatClass:

No

Quantity:

5

Unit of Measurement:

MG

MPN:

PZ0400-5MG

CAS:

857290-04-1