5.38437

MGAT2 Inhibitor, Cpd24d

• Synonym(s): MGAT2 Inhibitor, Cpd24d, 5-(N-(2,4-difluorophenyl)sulfamoyl)-7-(2-oxopyrrolidin-1-yl)-N-(4-(trifluoromethyl)phenyl)indoline-1-carboxamide , Acyl CoA:monoacylglycerol acyltransferase 2 inhibitor, Cpd24d
• Empirical Formula (Hill Notation): C₂₆H₂₁F₅N₄O₄S
• Molecular Weight: 580.53
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• assay: ≥98% (HPLC)
• Quality Level: 100
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 100 mg/mL
• storage temp.: 2-8°C

Description

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
MGAT2

Reversible: yes

Target IC₅₀: 3.4 nM for MGAT inhibition

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

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

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable