1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Acyltransferase

Acyltransferase

Diacylglycerol acyltransferase; Diglyceride acyltransferase; acyl-CoA:cholesterol acyltransferase; mono- acylglycerol acyltransferase

Acyltransferase (AT) catalyzes the transfer of an acyl moiety from acyl-coenzyme A (acyl-CoA) to an acceptor. Acyltransferases play important roles in the maintenance of homeostasis in the human body and have been linked to various diseases. The Acyltransferase family includes acyl-CoA:cholesterol AT (ACAT), diacylglycerol AT (DGAT), and monoacylglycerol AT (MGAT) for the metabolism of lipids.

ACAT (acyl-coenzyme A:cholesterol acyltransferase) is an intracellular enzyme that catalyzes the formation of cholesterol esters from cholesterol and fatty acyl-coenzyme A. In mammals, two isoenzymes, ACAT1 and ACAT2, encoded by two different genes, exist. ACATs play important roles in cellular cholesterol homeostasis in various tissues.

DGAT (acyl-CoA:diacylglycerol acyltransferase) is an integral membrane enzyme that catalyses the last step of triacylglycerol synthesis from diacylglycerol and acyl-CoA. DGAT activity resides mainly in two distinct membrane bound polypeptides, known as DGAT1 and DGAT2.

MGAT (acyl-CoA:monoacylglycerol acyltransferase) catalyzes the synthesis of diacylglycerol, the precursor of physiologically important lipids such as triacylglycerol and phospholipids. In the intestine, MGAT plays a major role in the absorption of dietary fat because resynthesis of triacylglycerol is required for the assembly of lipoproteins that transport absorbed fat to other tissues.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-107416R
    RHC 80267 (Standard)
    Inhibitor
    RHC 80267 (Standard) is the analytical standard of RHC 80267 (HY-107416). This product is intended for research and analytical applications. RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC50 of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC50 of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC).
    RHC 80267 (Standard)
  • HY-50670R
    DGAT-1 inhibitor 2 (Standard)
    Inhibitor
    DGAT-1 inhibitor 2 (Standard) is the analytical standard of DGAT-1 inhibitor 2 (HY-50670). This product is intended for research and analytical applications. DGAT-1 inhibitor 2 is an orally active DGAT-1 inhibitor with IC50 values of 15 nM and 9 nM for human DGAT-1 and rat DGAT-1, respectively. DGAT-1 inhibitor 2 increases ROS concentration, GRP78, and PERK protein abundance. DGAT-1 inhibitor 2 increases SREBF1, CPT1A, and MTTP mRNA in fatty acid-treated cells. DGAT-1 inhibitor 2 improves obesity.
    DGAT-1 inhibitor 2 (Standard)
  • HY-135505
    JTP-103237
    Inhibitor
    JTP-103237 is a MGAT2 inhibitor (IC50: 0.019 μM and 6.423 μM for hMGAT2 and hMGAT3 respectively). JTP-103237 modulates fat absorption, decreases plasma glucose levels and prevents diet-induced obesity.
    JTP-103237
  • HY-181564
    MGAT2-IN-7
    Inhibitor
    MGAT2-IN-7 is an orally active monoacylglycerol acyltransferase 2 (MGAT2) inhibitor. MGAT2-IN-7 is used for research on obesity and metabolic dysfunction-associated steatotic liver disease (MASLD).
    MGAT2-IN-7
  • HY-101722R
    Melinamide (Standard)
    Melinamide (Standard) is the analytical standard of Melinamide. This product is intended for research and analytical applications. Melinamide, an amide derivative of an unsaturated long-chain fatty acid, is an inhibitor of cholesterol absorption with an IC50 of 20.9 μM.
    Melinamide (Standard)
  • HY-N14525
    Glisoprenin A
    Inhibitor
    Glisoprenin A is a cholesterol acyltransferase (ACAT) inhibitor, and it can inhibit the formation of Appressorium on the hydrophobic surface of Magnaporthegrisea.
    Glisoprenin A
  • HY-107571R
    VULM 1457 (Standard)
    Inhibitor
    VULM 1457 (Standard) is the analytical standard of VULM 1457 (HY-107571). This product is intended for research and analytical applications. VULM 1457 is a potent inhibitor of cholesterol acyltransferase (acyl-CoA). VULM1457 significantly reduces production and secretion of adrenomedullin (AM) and down-regulates AM receptors on human hepatoblastic cells. VULM 1457 has remarkable hypolipidaemic activity and improves the overall myocardial ischaemia-reperfusion injury outcomes. VULM 1457 has the potential for the research of diabetes mellitus and hypercholesterolaemia.
    VULM 1457 (Standard)
  • HY-108341AR
    PF-06424439 methanesulfonate (Standard)
    Inhibitor
    PF-06424439 methanesulfonate (Standard) is the analytical standard of PF-06424439 (methanesulfonate) (HY-108341A). This product is intended for research and analytical applications. PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM. PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.
    PF-06424439 methanesulfonate (Standard)
  • HY-N14813
    Glisoprenin D
    Inhibitor
    Glisoprenin D is a cholesterol acyltransferase (ACAT) inhibitor, and it can inhibit the formation of Appressorium on the hydrophobic surface of Magnaporthegrisea.
    Glisoprenin D
  • HY-16266
    JNJ-DGAT1-A
    Inhibitor
    JNJ-DGAT1-A is a selective DGAT1 inhibitor. JNJ-DGAT1-A inhibits DGAT1 activity and TG synthesis.
    JNJ-DGAT1-A
  • HY-169085
    LRAT-IN-1
    Inhibitor
    LRAT-IN-1 (compound 1) is a retinol acyltransferase (LRAT) inhibitor (IC50=21.1 μM). LRAT-IN-1 provides anti-aging effects by inhibiting the esterification of retinol to form retinol esters, increasing the available retinol in the skin. Research on LRAT-IN-1 as an anti-aging ingredient in cosmetics.
    LRAT-IN-1
  • HY-N14574
    Glisoprenin C
    Inhibitor
    Glisoprenin C is a cholesterol acyltransferase (ACAT) inhibitor, and it can inhibit the formation of Appressorium on the hydrophobic surface of Magnaporthegrisea.
    Glisoprenin C
  • HY-107396R
    YM-750 (Standard)
    Inhibitor
    YM-750 (Standard) is the analytical standard of YM-750 (HY-107396). This product is intended for research and analytical applications. YM-750 is a potent acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor (IC50=0.18 μM). ACAT catalyzes the formation of cholesteryl esters from cholesterol and long-chain fatty-acyl-coenzyme A.
    YM-750 (Standard)
  • HY-N0631R
    Cornuside (Standard)
    Inhibitor
    Cornuside (Standard) is the analytical standard of Cornuside (HY-N0631). This product is intended for research and analytical applications. Cornuside is an iridoid glycoside with anti-allergic, anti-inflammatory, and neuroprotective activities. Cornuside exerts anti-allergic activity by downregulating the p38 MAPK, JNK, and NF-κB signaling pathways, and inhibits IgE-mediated histamine release from mast cells. Cornuside improves cognitive impairment in mice by inhibiting BACE1 activity (IC50 = 55.84 μg/mL) and enhancing ChAT activity. Cornuside inhibits LPS (HY-D1056)-induced inflammatory mediators, including iNOS, COX-2, PGE2, TNF-α, IL-6, and IL-1β, by suppressing NF-κB activation.
    Cornuside (Standard)
  • HY-105445R
    CP-113818 (Standard)
    Inhibitor
    CP-113818 (Standard) is the analytical standard of CP-113818 (HY-105445). This product is intended for research and analytical applications. CP-113818 is a potent cholesterol acyltransferase (ACAT) inhibitor. CP-113818 can be used for the research of Alzheimer's disease.
    CP-113818 (Standard)
  • HY-13215R
    Avasimibe (Standard)
    Inhibitor
    Avasimibe (Standard) is the analytical standard of Avasimibe. This product is intended for research and analytical applications. Avasimibe (CI-1011; PD-148515) is an orally active acyl coenzyme A-cholesterol acyltransferase (ACAT; also called SOAT)) inhibitor with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively. Avasimibe can be used for the research of prostate cancer.
    Avasimibe (Standard)
  • HY-100288
    RP 73163 Racemate
    RP 73163 Racemate is the racemate of RP 73163. RP 73163 is a potent ACAT inhibitor, with cholesterol lowering activity.
    RP 73163 Racemate
  • HY-W012946R
    2-Furoic acid (Standard)
    Inhibitor
    2-Furoic acid (Standard) is the analytical standard of 2-Furoic acid. This product is intended for research and analytical applications. 2-Furoic acid (Furan-2-carboxylic acid) is an organic compound produced through furfural oxidation. 2-Furoic acid exhibits hypolipidemic effet, lowers both serum cholesterol and serum triglyceride levels in rats.
    2-Furoic acid (Standard)
  • HY-100400AR
    K-604 dihydrochloride (Standard)
    Inhibitor
    K-604 (dihydrochloride) (Standard) is the analytical standard of K-604 (dihydrochloride). This product is intended for research and analytical applications. K-604 dihydrochloride is a potent and selective acyl-CoA:cholesterol acyltransferase 1 (ACAT-1) inhibitor with an IC50 of 0.45±0.06 μM.
    K-604 dihydrochloride (Standard)
  • HY-117466
    FR186054
    Inhibitor
    FR186054 is an oral active acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor with the IC50 of 99 nM. FR186054 shows hypocholesterolemic effect and can be used for study of hypercholesterolemia and atherosclerosis.
    FR186054
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