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PF-915275

PF-915275

Item no.	HY-18056-100mg
Manufacturer	MedChem Express
CASRN	857290-04-1
Amount	100 mg
Quantity options	100 mg 10 mM/1 mL 10 mg 50 mg 5 mg
Category	Metabolism Diabetes Inhibitors & Compound Libraries Small Molecules
Type	Inhibitors
Specific against	other
Purity	99.74
Citations	[1]Bhat BG, et al. 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 11 -hydroxysteroid dehydrogenase type 1, in cynomolgus monkeys. J Pharmacol Exp Ther. 2008 Jan;324(1):299-305.\|[2]Siu M, et al. N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3493-7.\|[3]Courtney R, et al. Modulation of 11beta-hydroxysteroid dehydrogenase (11betaHSD) activity biomarkers and pharmacokinetics of PF-00915275, a selective 11betaHSD1 inhibitor. J Clin Endocrinol Metab. 2008 Feb;93(2):550-6.
Smiles	N#CC1=CC=C(C2=CC=C(S(NC3=NC(N)=CC=C3)(=O)=O)C=C2)C=C1
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	857290-04-1
Shipping Condition	Room temperature
Available
Manufacturer - Type	Reference compound
Manufacturer - Applications	Metabolism-sugar/lipid metabolism
Manufacturer - Targets	11β-HSD
Shipping Temperature	Room Temperature
Storage Conditions	-20°C, 3 years; 4°C, 2 years (Powder)
Molecular Weight	350.39
Product Description	PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively[1][2][3].
Manufacturer - Research Area	Metabolic Disease
Solubility	DMSO: ≥ 31 mg/mL
Manufacturer - Pathway	Metabolic Enzyme/Protease
Clinical information	Phase 1

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HY-18056-100mg-safety-datasheet.pdf