| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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| S6971 | Ervogastat | Ervogastat (PF-06865571, DGAT2i) is a potent diacylglycerol acyltransferase 2 (DGAT2) inhibitor that reduces steatosis and hepatic triglyceride levels in non-alcoholic steatohepatitis (NASH). | ||
| S0359 | T863 (DGAT-3) | T863 (DGAT-3) is a potent, selective and orally active inhibitor of Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) tht acts on the acyl-CoA binding site of DGAT1 and inhibits DGAT1-mediated triacylglycerol formation in cells. |
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| S0820 | RP-64477 | RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT). This compound inhibits ACAT activity with IC50 of 113 nM, 503 nM, and 180 nM in human intestinal (CaCo-2), hepatic (HepG2) and monocytic (THP-1) cell assays, respectively. | ||
| S9162 | Rubimaillin | Rubimaillin (Mollugin), found in the Chinese medical plant Rubia cordifola, is a dual inhibitor of acetyl-CoA cholesterol acyltransferase 1 (ACAT1) and acetyl-CoA cholesterol acyltransferase 2 (ACAT2), but is more selective for the ACAT2 isozyme. | ||
| E0941 | K-604 dihydrochloride | K-604 dihydrochloride, a potent and selective inhibitor of Acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1), suppresses the development of atherosclerosis in an animal model without affecting plasma cholesterol levels. | ||
| S9921 | PF-06424439 Methanesulfonate |
PF-06424439 is a first orally bioavailable small-molecule inhibitor of DGAT2 with an IC50 of 14 nM. |
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| E7561 | Pradigastat | Pradigastat (LCQ-908) is a potent and selective inhibitor of DGAT1 with an IC50 of 57 nM in hDGAT1. It also inhibits OATP1B1, OATP1B3 , and OAT3 activity in a concentration-dependent manner, with an IC50 of 1.66 μM, 3.34 μM, and 0.973 μM, respectively. | ||
| S2187 | Avasimibe | Avasimibe inhibits ACAT with IC50 of 3.3 μM, also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9 μM, 13.9 μM and 26.5 μM, respectively. |
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| S7889 | Xanthohumol | Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. This compound inhibits diacylglycerol acyltransferase 1 (DGAT1) and DGAT2 with both IC50 of 40 μM. It is also a potent antiviral agent against a series of DNA and RNA viruses. This chemical induces growth inhibition and apoptosis in cancer cells. Phase 1. |
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| S3021 | Rimonabant (SR141716) | Rimonabant (SR141716) is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane, and it is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 that inhibits mycobacterial MmpL3. |
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