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 |
|---|---|---|---|---|
|
V73896 | Obeversen | 2304711-30-4 | Obeversen is a diacylglycerol acyltransferase 2 (DGAT-2) synthesis inhibitor. |
|
V73886 | P053 | 2748196-63-4 | P053 is a potent, noncompetitive and selective inhibitor of ceramide synthase 1 (CerS1) with IC50 of 0.5 μM. |
|
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. |
|
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. |
|
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. |
|
V73903 | PF-07202954 | 2639372-47-5 | PF-07202954 is a weakly basic DGAT2 inhibitor (antagonist) with IC50 of 10 nM for human DGAT2. |
|
V51508 | Phenylpyropene C | 419532-92-6 | Phenylpyropene C (S14-95) is a JAK/STAT coupling that can mediate the inhibition of IFN-γ-induced reporter gene expression (IC50=5.4~10.8 μM). |
|
V73901 | Pomonic acid | 13849-90-6 | Pomonic acid is a triterpene compound that can significantly inhibit the accumulation of cholesterol esters and inhibit the activity of acyl-CoA:cholesterol acyltransferase (ACAT). |
|
V4537 | Pradigastat (LCQ-908) | 956136-95-1 | Pradigastat (formerly also known as LCQ-908; LCQ908) is a novel, potent and orally bioavailablediacylglycerol acyltransferase 1 (DGAT1) inhibitor being developed for the treatment of familial chylomicronemia syndrome. |
|
V73910 | VULM 1457 | 228544-65-8 | VULM 1457 is a potent inhibitor of cholesterol acyltransferase (acyl-CoA). |
|
V73889 | YM-750 | 138046-43-2 | YM-750 is a potent acyl:cholesterol acyltransferase (ACAT) inhibitor (IC50=0.18 μM). |
|
V73902 | γ-Sanshool | 78886-65-4 | γ-Sanshool can be extracted from Zanthoxylum bungeanum. |
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