Biochem/physiol Actions

Target IC₅₀: 3.4 nM for MGAT inhibition

Reversible: yes

Primary TargetMGAT2

Cell permeable: yes

General description

A cell-permeable, bioavailable, indoline derivative that acts as a highly potent inhibitor of acyl CoA:monoacylglycerol acyltransferase 2 inhibitor (MGAT2, IC₅₀ = 3.4 nM). Displays good microsomal stability and desirable pharmacokinetic properties (F = 52%; AUC 0 - 8 h = 842 ng/h/ml). Effectively suppresses the elevation of plasma triacylglyceride levels after olive oil challenge in C57BL/6J mice (10 - 30 mg/kg; p.o.).

A cell-permeable, bioavailable, indoline derivative that acts as a highly potent inhibitor of acyl CoA:monoacylglycerol acyltransferase 2 inhibitor (MGAT2, IC₅₀ = 3.4 nM). Displays good microsomal stability and desirable pharmacokinetic properties (F = 52%; AUC 0 - 8 h = 842 ng/h/ml). Effectively suppresses the elevation of plasma triacylglyceride levels after olive oil challenge in C57BL/6J mice (10 - 30 mg/kg; p.o.).Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Sato, K., et al. 2015. J. Med. Chem.58, 3892.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)