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Acyltransferase

Other Metabolism Related Inhibitors

Dehydrogenase Transferase DPP Aminopeptidase Procollagen C Proteinase P450 (e.g. CYP17) Phospholipase (e.g. PLA) Factor Xa PDE DHFR

Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
S6971 Ervogastat (PF-06865571) Ervogastat (PF-06865571, DGAT2i) is a potent diacylglycerol acyltransferase 2 (DGAT2) inhibitor that reduces steatosis and hepatic triglyceride levels in non-alcoholic steatohepatitis (NASH).
S2187 Avasimibe (CI-1011) 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.
J Lipid Res, 2025, 66(8):100854
Hepatol Commun, 2025, 9(6)e0714
Nat Commun, 2024, 15(1):8301
Verified customer review of Avasimibe (CI-1011)
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.
J Virol, 2024, 98(11):e0110324
J Cell Sci, 2024, 137(20)jcs262162
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.
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.
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.
Oncotarget, 2025, 16:532-544
J Cell Sci, 2024, 137(20)jcs262162
Antiviral Res, 2022, 207:105416
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.
Biol Pharm Bull, 2025, 48(6):769-781
Toxicol Lett, 2023, 374:48-56
Int J Biol Sci, 2022, 18(4):1401-1414