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PF-915275
Catalog Number: orb611853
| Catalog Number | orb611853 |
|---|---|
| Category | Small Molecules |
| Description | PF-915275 is a potent and selective inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) (Ki ＜ 1 nM) with good preclinical pharmacokinetic properties.IC50 value: ＜ 1 nM (Ki)[2]Target: 11βHSD1in vitro: PF-915275 maintains potency in our cellular assay against human 11βHSD1 (HEK293, EC50 = 5 nM) and is selective against human 11βHSD2 (HEK293, 1.5% inhibition 10 μM). PF-915275 displays only weak affinity for the rodent choline transporter (Ki = 9.6 μM) and the hamster melatonin MT3 receptor (Ki = 9.6 μM) 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 Number | [857290-04-1] |
| MW | 350.3943 |
| SMILES | NC1N=C(NS(C2C=CC(C3C=CC(C#N)=CC=3)=CC=2)(=O)=O)C=CC=1 |
| Formula | C18H14N4O2S |
| Note | For research use only |
| Expiration Date | 12 months from date of receipt. |
PF-915275 [orb1307890]
97.69%
857290-04-1
350.39
C18H14N4O2S
2 mg, 50 mg, 5 mg, 10 mg, 25 mg, 100 mg, 500 mg, 1 mg, 1 ml x 10 mm (in DMSO)
