Product Details
Product Name:
– PF-915275
Catalog Number:
– D24093
Field of Application:
– PF-915275 is a potent and selective inhibitor of human 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) (Ki ? 1 nM) with good preclinical pharmacokinetic properties.IC50 value: ? 1 nM (Ki)[2]Target: 11?HSD1in vitro: PF-915275 maintains potency in our cellular assay against human 11?HSD1 (HEK293, EC50 = 5 nM) and is selective against human 11?HSD2 (HEK293, 1.5% inhibition 10 ?M). PF-915275 displays only weak affinity for the rodent choline transporter (Ki = 9.6 ?M) and the hamster melatonin MT3 receptor (Ki = 9.6 ?M) in the Cerep Bioprint screening panel. PF-915275 has good in vitro pharmacokinetic properties. In particular, PF-915275 is categorized as a low clearance compound (liver microsome assays) with high permeability (Caco2 assay). [2]in vivo: As a prelude to in vivo studies with PF-915275, the rat pharmacokinetic properties of this compound were determined. PF-915275 has an excellent pharmacokinetic profile characterized by low clearance, long half-life and good oral bioavailability. [2]
CAS:
– [857290-04-1]
Formular:
– C18H14N4O2S
SMILES:
– NC1N=C(NS(C2C=CC(C3C=CC(C#N)=CC=3)=CC=2)(=O)=O)C=CC=1
