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PF-915275 (C005B-432405)

Catalog No.
C005B-432405
Mfr. No.
PZ0400-5MG
Mfr. Name
Sigma-Aldrich
Qty/UOM
5
UOM
MG
Price: $234.68
List Price: $260.76

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 IC 50 = 5 nM using human 11ß-HSD1-transfected HEK293

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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.

UPC:
51422101
Condition:
New
Availability:
3-5 Days
Weight:
1.00 Ounces
HazmatClass:
No
MPN:
PZ0400-5MG
CAS:
857290-04-1

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