EC Number   |
Inhibitors |
Structure |
|---|
   2.3.1.22 | (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 |
   |
| 2.3.1.22 | (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 |
|
| 2.3.1.22 | (1S)-4'-(2-cyclopropyl-3H-pyrrol-4-yl)-5'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-5-(4,4,4-trifluorobutoxy)-2,3-dihydro-1'H-spiro[indene-1,2'-pyridin]-6'(3'H)-one |
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis |
|
| 2.3.1.22 | (3R)-N-(2,4-difluorophenyl)-3-ethyl-3-methyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide |
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis |
|
| 2.3.1.22 | (6S)-4-(4-methylphenyl)-2-oxo-N-[4-(1H-tetrazol-5-yl)phenyl]-6-[4-(4,4,4-trifluorobutoxy)phenyl]-6-(trifluoromethyl)-1,2,5,6-tetrahydropyridine-3-carboxamide |
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis |
|
| 2.3.1.22 | (6S)-4-(5-cyclopropyl-1,3-thiazol-2-yl)-6-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-3-(5-oxo-4,5-dihydro-1H-tetrazol-1-yl)-6-(trifluoromethyl)-5,6-dihydropyridin-2(1H)-one |
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis |
|
| 2.3.1.22 | (6S)-4-(5-cyclopropylthiophen-2-yl)-3-(2,5-dihydro-1H-tetrazol-5-yl)-6-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-6-(trifluoromethyl)-5,6-dihydropyridin-2(1H)-one |
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis |
|
| 2.3.1.22 | (6S)-4-[4-(difluoromethyl)phenyl]-6-[2-fluoro-4-[(6,6,6-trifluorohexyl)oxy]phenyl]-N-(methanesulfonyl)-2-oxo-6-(trifluoromethyl)-1,2,5,6-tetrahydropyridine-3-carboxamide |
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis |
|
| 2.3.1.22 | 1-(2,2,3,3,3-pentafluoropropyl)piperidin-4-yl 5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxoimidazolidin-1-yl)-2,3-dihydro-1H-indole-1-carboxylate |
ex hibits more than 100fold selectivity over human MGAT3, human DGAT1, and human DGAT2 |
|
| 2.3.1.22 | 1-(2,2,3,3,3-pentafluoropropyl)piperidin-4-yl 5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxoimidazolidin-1-yl)-2,3-dihydro-1H-indole-1-carboxylate |
- |
|
