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-117832
    Pyripyropene A
    Inhibitor 98.16%
    Pyripyropene A is an orally active, potent and selective sterol O-acyltransferase 2 (SOAT2)/acyl-coenzyme A:cholesterol acyltransferase 2 (ACAT2) inhibitor, with an IC50 of 0.07 µM. Pyripyropene A attenuates hypercholesterolemia and atherosclerosis in vivo.
    Pyripyropene A
  • HY-117656
    ESI-05
    Inhibitor 99.78%
    ESI-05 is a specific exchange proteins directly activated by cAMP 2 (EPAC2) inhibitor. ESI-05 inhibits cAMP-mediated EPAC2 GEF activity with an IC50 of 0.43 μM. ESI-05 can be used for the research of diabetes, insulin secretion and neurological disorders.
    ESI-05
  • HY-107572
    PD 128042
    Inhibitor 99.97%
    PD 128042 (CI 976) is a potent, orally active, and selective inhibitor of ACAT (acyl coenzyme A:cholesterol acyltransferase) with an IC50s of 73 nM. PD 128042 is also a potent LPAT (lysophospholipid acyltransferase) inhibitor. PD 128042 inhibits Golgi-associated LPAT activity (IC50=15 μM). PD 128042 inhibits multiple membrane trafficking steps, including ones found in the endocytic and secretory pathway.
    PD 128042
  • HY-P5282
    ApoA-I mimetic peptide
    Activator 98.37%
    ApoA-I mimetic peptide (PVLDLFRELLNELLEALKQKLK) has good lecithin:cholesterol acyl transferase (LCAT) activation potency. ApoA-I mimetic peptide can be used for synthesis of peptide/lipid complex.
    ApoA-I mimetic peptide
  • HY-16278
    Pradigastat
    Inhibitor 98.88%
    Pradigastat (LCQ-908) is a selective and orally effective diacylglyceryl acyltransferase 1 (DGAT1) inhibitor with IC50 at 0.157 µM. Pradigastat is primarily used to study diseases associated with abnormal triglyceride metabolism. Pradigastat has anti-obesity and anti-diabetic effects. Pradigastat inhibited BCRP, OATP1B1, OATP1B3 and OAT3 activities with IC50 of 5 µM, 1.66µM, 3.34µM and 0.973µM, respectively. In addition, Pradigastat has antiviral activity and can inhibit hepatitis C virus replication in vitro.
    Pradigastat
  • HY-153855
    Zamaporvint
    Inhibitor 99.76%
    Zamaporvint (RXC004) is an orally active and selective inhibitor of Wnt. Zamaporvint targete membrane-bound o-acyltransferase Porcupine and inhibited Wnt ligand palmitoylation, secretion, and pathway activation. Zamaporvint displays a favorable pharmacokinetic profile and shows potent antiproliferative effects in Wnt ligand-dependent colorectal and pancreatic cell lines. Zamaporvint possesses multiple antitumor mechanisms and can be used in cancer research.
    Zamaporvint
  • HY-W018026
    Oxfenicine
    Inhibitor 99.76%
    Oxfenicine (L-p-Hydroxyphenylglycine) is an orally active carnitine palmitoyltransferase-1 inhibitor. Oxfenicine inhibits the oxidation of fatty acids in the heart, protecting cardiac tissue from necrotic damage during ischemia, and also has an inhibitory effect on cardiac tissue apoptosis. In addition, Oxfenicine promotes lipolysis in a high-fat diet rat model. Oxfenicine can be used in the study of cardiovascular and metabolic diseases.
    Oxfenicine
  • HY-15497
    AZD7687
    Inhibitor 99.80%
    AZD7687 is a potent, selective, reversible and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor with an IC50 of 80 nM for human DGAT1. AZD7687 can be used for type 2 diabetes mellitus and obesity research.
    AZD7687
  • HY-W012946
    2-Furoic acid
    Inhibitor 99.98%
    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
  • HY-110381
    JNJ-DGAT2-A
    Inhibitor 98.26%
    JNJ-DGAT2-A is a selective diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 value of 0.14 μM in human DGAT2-expressing Sf9 insect cell membranes. JNJ-DGAT2-A can be used for the research of triglyceride (TG) synthesis.
    JNJ-DGAT2-A
  • HY-12425
    DGAT1-IN-1
    Inhibitor ≥98.0%
    DGAT1-IN-1 (example 1) is a DGAT1 inhibitor. DGAT1-IN-1 can be useful in the study of a disease, disorder or condition modulated by DGATl inhibition, such as obesity-related disorders, type 2 diabetes, or diabetes-related disorders.
    DGAT1-IN-1
  • HY-103479
    GOAT-IN-1
    Inhibitor 99.38%
    GOAT-IN-1 is an inhibitor of ghrelin O-acyltransferase (GOAT), which could be useful for the prophylaxis or treatment of obesity, diabetes, hyperlipidemia, metabolic, non-alcoholic fatty liver, steatohepatitis, sarcopenia, appetite control, alcohol/narcotic dependence, Alzheimer’s disease, Parkinson’s disease, cerebrovascular dementia, cerebral apoplexy, cerebral infarction, cardic disease, some kind of tumors.
    GOAT-IN-1
  • HY-136282
    OGT-IN-2
    Inhibitor 99.82%
    OGT-IN-2 (compound 4) is a potent O-GlcNAc transferase (OGT) inhibitor, with IC50 values of 30 and 53 μM for sOGT and ncOGT, respectively.
    OGT-IN-2
  • HY-101857
    TP-020
    Inhibitor 99.94%
    TP-020 (MGAT2-IN-1) is an orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC50 of 7.8 and 2.4 nM for human and mouse MGAT2, respectively.
    TP-020
  • HY-132924
    BMS-963272
    Inhibitor 99.92%
    BMS-963272 is an orally active and selective MGAT2 inhibitor (IC50 = 7.1 nM), used for the study of metabolic disorders and inflammatory diseases.
    BMS-963272
  • HY-N4193
    Glabrol
    Inhibitor 99.95%
    Glabrol (Compound 1), One isoprenyl flavonoid was isolated from ethanol extract of licorice roots, is a potent and non-competitive Acyl-coenzyme A: cholesterol acyltransferase (ACAT) inhibitor with an IC50 value of 24.6 μM for rat liver microsomal ACAT activity.
    Glabrol
  • HY-133968
    24-Methylenecholesterol
    Activator 99.48%
    24-Methylenecholesterol (Ostreasterol) is a regulator targeting acyl-CoA cholesterol acyltransferase (ACAT) with anti-aging and neuroprotective effects. 24-Methylenecholesterol mimics the effects of nerve growth factor (NGF), can extend yeast lifespan through an anti-oxidative stress mechanism, and exhibits neuroprotective activity in PC12 cells. 24-Methylenecholesterol can reduce intracellular reactive oxygen species (ROS) and malondialdehyde (MDA) levels, activate anti-oxidative stress pathways (such as UTH1, SOD-related genes), and promote synaptic growth.
    24-Methylenecholesterol
  • HY-50861
    AZD3988
    Inhibitor 99.89%
    AZD3988 is an orally active diacylglycerol acyl transferase-1 (DGAT-1) inhibitor. AZD3988 has excellent DGAT-1 (human) potency with an IC50 value of 0. 6 nM. AZD3988 can be used for the research of metabolic diseases such as diabetes, obesity.
    AZD3988
  • HY-156259
    PF-07202954
    Inhibitor 98.82%
    PF-07202954 is a weakly basic DGAT2 inhibitor with an IC50 of 10 nM for human DGAT2. PF-07202954 lowers liver triglyceride content in a Western-diet-fed rat model.
    PF-07202954
  • HY-115938
    BEC2
    Inhibitor ≥98.0%
    BEC2 is an ester derivative of Baicalin, with good lipid-lowering activity. BEC2 can direct activate the carnitine palmitoyltransferase 1A (CPT1A).
    BEC2
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