A potent and selective inhibitor of DGAT-1 (IC50 = 19 nM); has high oral bioavailability (100%) in rats with a moderate half-life of 6.8 hours; significantly blocks an increase in plasma triglyceride levels following a corn oil bolus in rats

PF-04620110 – 10 mg

Brand:
Cayman
CAS:
1109276-89-2
Storage:
-20
UN-No:
Non-Hazardous - /

Acyl-CoA:diacylglycerol acyltransferase-1 (DGAT-1) catalyzes the final committed step in the biosynthesis of triglycerides and has potential roles in obesity, diabetes, and atherosclerosis.{12021,15816,10960} PF-04620110 is a potent inhibitor of DGAT-1 (IC50 = 19 nM) that is without effect on DGAT-2.{26854} It has high oral bioavailability (100%) in rats, with a moderate half-life of 6.8 hours.{26854} PF-04620110 significantly blocks an increase in plasma triglyceride levels following a corn oil bolus in rats.{26854}  

 

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Description

A potent and selective inhibitor of DGAT-1 (IC50 = 19 nM); has high oral bioavailability (100%) in rats with a moderate half-life of 6.8 hours; significantly blocks an increase in plasma triglyceride levels following a corn oil bolus in rats

Formal name: trans-4-[4-(4-amino-7,8-dihydro-5-oxopyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl]-cyclohexaneacetic acid

Synonyms: 

Molecular weight: 396.4

CAS: 1109276-89-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Sterol Biosynthesis||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Dyslipidemias

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