Product Name :
MGAT2-IN-2
Description:
MGAT2-IN-2 is a potent and selective acyl CoA:monoacylglycerol acyltransferase 2 (MGAT2) inhibitor with an IC50 of 3.4 nM.
CAS:
1710630-11-7
Molecular Weight:
580.53
Formula:
C26H21F5N4O4S
Chemical Name:
5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxopyrrolidin-1-yl)-N-[4-(trifluoromethyl)phenyl]-2,3-dihydro-1H-indole-1-carboxamide
Smiles :
O=C1CCCN1C1=CC(=CC2CCN(C=21)C(=O)NC1C=CC(=CC=1)C(F)(F)F)S(=O)(=O)NC1=CC=C(F)C=C1F
InChiKey:
RGDHGNPUKLLPLT-UHFFFAOYSA-N
InChi :
InChI=1S/C26H21F5N4O4S/c27-17-5-8-21(20(28)13-17)33-40(38,39)19-12-15-9-11-35(24(15)22(14-19)34-10-1-2-23(34)36)25(37)32-18-6-3-16(4-7-18)26(29,30)31/h3-8,12-14,33H,1-2,9-11H2,(H,32,37)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
MGAT2-IN-2 is a potent and selective acyl CoA:monoacylglycerol acyltransferase 2 (MGAT2) inhibitor with an IC50 of 3.4 nM.|Product information|CAS Number: 1710630-11-7|Molecular Weight: 580.53|Formula: C26H21F5N4O4S|Chemical Name: 5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxopyrrolidin-1-yl)-N-[4-(trifluoromethyl)phenyl]-2,3-dihydro-1H-indole-1-carboxamide|Smiles: O=C1CCCN1C1=CC(=CC2CCN(C=21)C(=O)NC1C=CC(=CC=1)C(F)(F)F)S(=O)(=O)NC1=CC=C(F)C=C1F|InChiKey: RGDHGNPUKLLPLT-UHFFFAOYSA-N|InChi: InChI=1S/C26H21F5N4O4S/c27-17-5-8-21(20(28)13-17)33-40(38,39)19-12-15-9-11-35(24(15)22(14-19)34-10-1-2-23(34)36)25(37)32-18-6-3-16(4-7-18)26(29,30)31/h3-8,12-14,33H,1-2,9-11H2,(H,32,37)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|MGAT2-IN-2 (Compound 24d) exhibits potent MGAT2 inhibitory activity with an IC50 value of 3.4 nM and a ligand lipophilicity efficiency (LLE) value of 5.4. MGAT2-IN-2 (Compound 2) exhibits time-dependent inhibition (TDI) of cytochrome P450 3A4 (CYP3A4). Preincubation of MGAT2-IN-2 with microsomes leads to a significant loss of the activity of CYP3A4 relative to that under a condition without preincubation.|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.Mevastatin Description Pharmacokinetic studies reveal that MGAT2-IN-2 displays a high plasma concentration (AUC0-8h=842 ng•h/mL) and favorable oral bioavailability (F=52%), which are probably driven by the improved stability against oxidative metabolism and hydrolysis.Trypsin-EDTA supplier For evaluating the in vivo efficacy, MGAT2-IN-2 is examined for its effect on hypertriglyceridemia during oral fat tolerance test (OFTT) using C57BL/6J mice.PMID:32602761 To inhibit the hydrolysis of plasma triacylglycerol (TG) by lipoprotein lipase (LPL), mice are pretreated with an LPL inhibitor, Pluronic F127, permitting measurement of the accumulation of plasma TG following olive oil administration. MGAT2-IN-2 and vehicle are administered 6 h before the oral olive oil load, and plasma chylomicron TG concentrations are monitored for 4 h. MGAT2-IN-2 effectively and dose-dependently suppresses plasma TG elevation after olive oil challenge. The TG-lowering effect of MGAT2-IN-2 is significant (pProducts are for research use only. Not for human use.|