Acyl-coenzyme A (acyl-CoA) transfers an acyl moiety to an acceptor through the action of the enzyme acyltransferase (AT). Acyltransferases have been connected to a number of diseases and are crucial for the maintenance of homeostasis in the human body. The acyl-CoA:cholesterol AT (ACAT), diacylglycerol AT (DGAT), and monoacylglycerol AT (MGAT) are members of the acyltransferase family, which is involved in the metabolism of lipids.
ACAT (acyl-coenzyme A:cholesterol acyltransferase) is an intracellular enzyme that facilitates the conversion of cholesterol and fatty acyl-coenzyme A into cholesterol esters. ACAT1 and ACAT2, two isoenzymes that are encoded by separate genes, are found in mammals. In many tissues, ACATs are crucial for maintaining cellular cholesterol homeostasis.
DGAT (acyl-CoA:diacylglycerol acyltransferase) is an integral membrane enzyme that catalyzes the final step of triacylglycerol synthesis from diacylglycerol and acyl-CoA. Two distinct membrane-bound polypeptides, known as DGAT1 and DGAT2, are where the majority of the DGAT activity is found.
MGAT (acyl-CoA:monoacylglycerol acyltransferase) catalyzes the synthesis of diacylglycerol, the precursor of physiologically significant lipids like triacylglycerol and phospholipids. Because the assembly of the lipoproteins that carry absorbed fat to other tissues depends on the resynthesis of triacylglycerol, MGAT plays a significant role in the absorption of dietary fat in the intestine.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V103452 | Cyano-myracrylamide | 2801702-34-9 | Cyano-myracrylamide is an inhibitor of zinc finger DHHC domain-containing palmitoyltransferase 20 (zDHHC20) with IC50 of 1.35 µM. |
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V19715 | DGAT1-IN-1 | 1449779-49-0 | DGAT1-IN-1 is a effective DGAT1 inhibitor (antagonist) with IC50 lower than 10nM (measured by lysate of Hep3B cells overexpressing DGAT1). |
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V94828 | DGAT2-IN-3 | 3037141-61-7 | DGAT2-IN-3 (Compound 9) is a DGAT2 inhibitor with IC50 value of 0.4 nM. |
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V97349 | Diacylglycerol acyltransferase inhibitor-2 | 2186700-48-9 | Diacylglycerol acyltransferase inhibitor-2 (Example 8) is a diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 3.7 nM. |
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V73885 | F-1394 | 162490-89-3 | F-1394 is an orally bioavailable acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor that can suppress dietary cholesterol absorption in mice. |
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V73908 | GSK2973980A | 2219321-25-0 | GSK2973980A is a potent, selective acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) inhibitor (antagonist) with IC50 of 3 nM. |
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V73904 | Ilexoside | 129095-76-7 | Ilexoside XLVIII is an acyl-CoA cholesterol acyltransferase (ACAT) inhibitor. |
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V97225 | IONIS-DGAT 2Rx | 2091332-22-6 | IONIS-DGAT 2Rx (ION-224) is a DGAT2 inhibitor with potential for studying atherosclerosis. |
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V97351 | IONIS-DGAT 2Rx sodium | IONIS-DGAT 2Rx (ION-224) sodium is a DGAT2 inhibitor with potential for the study of atherosclerosis. | |
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V84707 | JTP-103237 | 1883864-16-1 | |
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V93073 | KY-455 | 178469-71-1 | KY-455 is a novel acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor. |
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V87269 | LDL-IN-1 | 615264-52-3 | LDL-IN-1 (Compound 1) is an antioxidant with anti-copper-mediated LDL oxidation activity (IC50 = 52 μM). |
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V87272 | LDL-IN-4 | 615264-62-5 | LDL-IN-4 inhibits the activity of human acyl-CoA: cholesterol acyltransferase-1 and -2. |
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V73896 | Obeversen | 2304711-30-4 | Obeversen is a diacylglycerol acyltransferase 2 (DGAT-2) synthesis inhibitor. |
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V87267 | Oleyl anilide | 5429-85-6 | Oleyl anilide (Oleic acid anilide) is a toxic substance found in certain toxic oil depots and is associated with toxic oil syndrome (TOS). |
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V73886 | P053 | 2748196-63-4 | P053 is a potent, noncompetitive and selective inhibitor of ceramide synthase 1 (CerS1) with IC50 of 0.5 μM. |
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V73909 | Pactimibe sulfate (CS-505) | 608510-47-0 | Pactimibe sulfate (CS-505) is an ACAT1/2 dual (bifunctional) inhibitor (antagonist) with IC50s of 4.9 μM for ACAT1 and 3.0 μM for ACAT2. |
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V73888 | PD 128042 (CI 976) | 114289-47-3 | PD 128042 (CI 976) is a potent, orally bioactive, selective inhibitor of ACAT (acyl-CoA:cholesterol acyltransferase) with IC50 of 73 nM. |
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V4472 | PF-06471553 | 1808094-07-6 | PF-06471553 (PF06471553) is a novel, potent, selective and orally bioavailablemonoacylglycerol acyltransferase 3 (MGAT3)inhibitor with the potential to treat insulin resistance, diabetes, dyslipidemia, and hepatic steatosis. |
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V73903 | PF-07202954 | 2639372-47-5 | PF-07202954 is a weakly basic DGAT2 inhibitor (antagonist) with IC50 of 10 nM for human DGAT2. |
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