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Literature summary for 2.3.1.22 extracted from

  • Mochida, T.; Take, K.; Maki, T.; Nakakariya, M.; Adachi, R.; Sato, K.; Kitazaki, T.; Takekawa, S.
    Inhibition of MGAT2 modulates fat-induced gut peptide release and fat intake in normal mice and ameliorates obesity and diabetes in ob/ob mice fed on a high-fat diet (2020), FEBS Open Bio, 10, 316-326 .
    View publication on PubMedView publication on EuropePMC
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Inhibitors

Inhibitors Comment Organism Structure
(1r,4r)-4-([[(3,3,4,4,4-pentafluoro-2-methylbutan-2-yl)oxy]carbonyl]amino)cyclohexyl 5-[(4-chloro-2,6-difluorophenyl)sulfamoyl]-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indole-1-carboxylate compound shows strong selectivity for MGAT2 over DGAT1, DGAT2 and ACAT1 Homo sapiens
(1r,4r)-4-([[(3,3,4,4,4-pentafluoro-2-methylbutan-2-yl)oxy]carbonyl]amino)cyclohexyl 5-[(4-chloro-2,6-difluorophenyl)sulfamoyl]-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indole-1-carboxylate compound inhibits elevation of plasma triglyceride in mice challenged with an oil-supplemented liquid meal. Oil challenge stimulates the secretion of hormones peptide tyrosine-tyrosine and glucagon-like peptide-1 into the bloodstream, and these responses are augmented in mice pretreated with the inhibitor. Administration of the compound to high-fat diet-fed ob/ob mice for 5 weeks suppresses food intake and body weight gain and inhibits elevation of glycated hemoglobin Mus musculus

Organism

Organism UniProt Comment Textmining
Homo sapiens Q3SYC2
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-
Mus musculus Q80W94
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-

Source Tissue

Source Tissue Comment Organism Textmining

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000085
-
 pH not specified in the publication, temperature not specified in the publication Mus musculus (1r,4r)-4-([[(3,3,4,4,4-pentafluoro-2-methylbutan-2-yl)oxy]carbonyl]amino)cyclohexyl 5-[(4-chloro-2,6-difluorophenyl)sulfamoyl]-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indole-1-carboxylate
0.0000081
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens (1r,4r)-4-([[(3,3,4,4,4-pentafluoro-2-methylbutan-2-yl)oxy]carbonyl]amino)cyclohexyl 5-[(4-chloro-2,6-difluorophenyl)sulfamoyl]-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indole-1-carboxylate