An orally bioavailable inhibitor of DGAT-2 (IC50 = 14 nM); selective for DGAT-2 over the related acyltransferases DGAT-1

PF-06424439 – 500 µg

Brand:
Cayman
CAS:
1469284-79-4
Storage:
-20
UN-No:
Non-Hazardous - /

PF-06424439 is an orally bioavailable inhibitor of diacylglycerol acyltransferase 2 (DGAT-2; IC50 = 14 nM).{46032} It is selective for DGAT-2 over the related acyltransferases DGAT-1, MGAT-2, and MGAT-3 (IC50s = >50 μM). PF-06424439 (0.1-10 mg/kg) reduces plasma triglyceride levels in sucrose-fed rats in a dose-dependent manner. It also reduces plasma levels of cholesterol and triglycerides as well as hepatic triglycerides in LDL receptor knockout mice fed a high-fat, high-cholesterol diet when administered at a dose of 60 mg/kg per day.  

 

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Description

An orally bioavailable inhibitor of DGAT-2 (IC50 = 14 nM); selective for DGAT-2 over the related acyltransferases DGAT-1, MGAT-2, and MGAT-3 (IC50s = >50 μM); reduces plasma triglyceride levels in sucrose-fed rats in a dose-dependent manner from 0.1-10 mg/kg; reduces plasma levels of cholesterol and triglycerides as well as hepatic triglycerides in LDL receptor knockout mice fed a high-fat, high-cholesterol diet at 60 mg/kg per day

Formal name: [(3R)-1-[2-[1-(4-chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-methanone, monomethanesulfonate

Synonyms: 

Molecular weight: 536

CAS: 1469284-79-4

Purity: ≥98%

Formulation: A crystalline solid

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

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