PF-915275
Biochem/physiol Actions
PF-915275 is an orally active, potent and selective 11beta-hydroxysteroid dehydrogenase type 1 (11ß-HSD1, HSD11B1) inhibitor (human 11ß-HSD1 Ki <1 nM; cellular IC50 = 5 nM using human 11ß-HSD1-transfected HEK293) with reduced potency toward non-human species (human/monkey/dog hepatocytes EC50 = 20/100/120 nM; mouse 11ß-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.
| Colour | white to beige |
|---|---|
| Quality Level | 100 |
| Manufacturer | SIGMA-ALDRICH |
| Storage Temp. | room temp |
| Solubility | DMSO: 2 mg/mL, clear |
| Form | powder |
| Assay | ≥98% (HPLC) |
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