| Description | MGAT2-IN-2 is a potent inhibitor of acyl CoA:monoacylglycerol acyltransferase 2 (MGAT2) (IC50 of 3.4 nM). |
| In vitro | MGAT2-IN-2 exhibits potent MGAT2 inhibitory activity with an IC50 value of 3.4 nM and a ligand lipophilicity efficiency (LLE) value of 5.4[1]. |
| In vivo | Effect of MGAT2-IN-2 on plasma TG is elevated during the oral fat tolerance test in C57BL/6J mice. MGAT2-IN-2 (3, 10 and 30 mg/kg) is orally administered 6 h prior to oil challenge. |
| Target activity | MGAT2:3.4 nM |
| molecular weight | 580.53 |
| Molecular formula | C26H21F5N4O4S |
| CAS | 1710630-11-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Sato K, et al. Discovery of a Novel Series of N-Phenylindoline-5-sulfonamide Derivatives as Potent, Selective, and Orally Bioavailable Acyl CoA:Monoacylglycerol Acyltransferase-2 Inhibitors. J Med Chem. 2015 May 14;58(9):3892-909. 2. Sato K, et al. Optimization of a novel series of N-phenylindoline-5-sulfonamide-based acylCoA:monoacylglycerol acyltransferase-2 inhibitors: Mitigation of CYP3A4 time-dependent inhibition and phototoxic liabilities. Bioorg Med Chem. 2015 Aug 1;23(15):4544-60. |