Acyltransferase Inhibitor

GOAT-IN-1 (Standard) is the analytical standard of GOAT-IN-1 (HY-103479). This product is intended for research and analytical applications. 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.

LDL-IN-4 (Compound 2) inhibits human acyl-CoA:cholesterol acyltransferase-1 and -2 activities. LDL-IN-4 inhibits copper-mediated low density lipoprotein (LDL) oxidation, with an IC₅₀ of 3 μM. LDL-IN-4 has anti-atherosclerotic biological activity.

Avasimibe sodium (CI-1011 sodium; PD-148515 sodium) 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 sodium can be used for the research of prostate cancer.

IWP-12 (Standard) is the analytical standard of IWP-12 (HY-107570). This product is intended for research and analytical applications. IWP-12 is a potent inhibitor of porcupine (PORCN) and inhibits cell-autonomous Wnt signaling with an IC₅₀ of 15 nM.

KY-455 is a novel inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT). KY-455 inhibita rabbit intestinal, hepatic, macrophage and adrenal ACAT with IC₅₀ values of 0.4, 0.9, 2.9 and 4.1 μmol/L, respectively.

Helminthosporol is a natural plant growth-regulator that can promote the growth of rice and lettuce seedlings. Helminthosporol can also inhibit the activity of acyl-CoA: cholesterol acyltransferase (ACAT) in rat liver microsomes and the synthesis of cholesterol esters in macrophages.

Pradigastat (Standard) is the analytical standard of Pradigastat. This product is intended for research and analytical applications. 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.

Roselipin 2B inhibits diacylglycerol acyltransferases (DGAT) of rat hepatic microcosm.

Purpactin C is a cholesterol acyltransferase (ACAT) inhibitor.

Pactimibe (sulfate) (Standard) is the analytical standard of Pactimibe (sulfate) (HY-100401A). This product is intended for research and analytical applications. Pactimibe sulfate (CS-505) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe sulfate (CS-505) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively. Pactimibe sulfate (CS-505) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe sulfate (CS-505) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe sulfate (CS-505) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity.

Gypsetin can inhibit acylcoenzyme A, cholesterol acyltransferase (ACAT) activity, inhibit rat liver microbody ACAT with an IC₅₀ of 18 μM, and its action is competitive with oleoyl-COA substrate, K_i value is 5.5 μM. Gypsetin also inhibits Oleic acid from forming cholesterol esters with an IC₅₀ of 0.65 μM.

ALCAT1-IN-1 is an ALCAT1 inhibitor.ALCAT1-IN-1 can be used for the research of aging and age-related diseases.

PF-06471553 (Standard) is the analytical standard of PF-06471553 (HY-108339). This product is intended for research and analytical applications. PF-06471553 is a potent, selective and orally available monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC₅₀ of 92 nM.

Purpactin A is a cholesterol acyltransferase (ACAT) inhibitor found in Pen. Purpurogenum FO-6.

RP 70676 (Standard) is the analytical standard of RP 70676 (HY-101576). This product is intended for research and analytical applications. RP 70676 is a potent inhibitor of ACAT, with IC50 of 25 and 44 nM for rat and rabbit ACAT.

Roselipin 1A inhibits diacylglycerol acyltransferases (DGAT) of rat hepatic microcosm.

TP-020 (Standard) (MGAT2-IN-1 (Standard)) is the analytical standard of TP-020 (HY-101857). This product is intended for research and analytical applications. TP-020 (MGAT2-IN-1), a chemical probe, is an orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC₅₀ of 7.8 and 2.4 nM for human and mouse MGAT2, respectively.

PF-06424439 (Standard) is the analytical standard of PF-06424439 (HY-108341). This product is intended for research and analytical applications. PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC₅₀ of 14 nM. PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.

MGAT2-IN-6 (Compound 23AX) is an orally active MGAT2 inhibitor. MGAT2-IN-6 reduces triglyceride levels and liver fibrosis. MGAT2-IN-6 can be used in the research of metabolic dysfunction-associated fatty liver disease.

A 922500 (Standard) is the analytical standard of A 922500 (HY-10038). This product is intended for research and analytical applications. A 922500 (DGAT-1 Inhibitor 4a) is a potent, selective, and orally bioavailable diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50s of 9 and 22 nM against human and mouse DGAT-1, respectively.