Acyltransferase Inhibitor

FR-190809 is a potent, nonadrenotoxic, orally efficacious acyl-CoA:cholesterol O-acyltransferase (ACAT) inhibitor, with an IC₅₀ of 45 nM.

Diacylglycerol acyltransferase inhibitor-2 (Example 8) is an inhibitor of Diacylglycerol Acyl Transferase 2 (DGAT2) with an IC₅₀ value of 3.7 nM.

Obeversen sodium is an antisense oligonucleotide that inhibits the synthesis of Diacylglycerol acyltransferase 2 (DGAT-2). Obeversen sodium can be used in the research of nonalcoholic fatty liver disease.

ACAT-IN-4 hydrochloride (Example 208) is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. ACAT-IN-4 hydrochloride inhibits NF-κB mediated transcription.

Oleyl anilide (Oleic acid anilide) is a toxic agent found in some stocks of toxic oil, which is associated with toxic oil syndrome (TOS). Oleyl anilide is an inhibitor of acyl-coenzyme A:cholesterol acyltransferase (ACAT) (IC₅₀: 26 µM).

Ilexoside XLVIII is an acyl CoA cholesteryl acyl transferase (ACAT) inhibitor. Ilexoside XLVIII is a triterpene saponin isolated from an aqueous extract of the leaves of Ilex kudincha.

Amidepsine D is a fungal metabolite isolated from the culture broth of Humicola sp. FO-2942 that inhibits Diacylglycerol acyltransferases (DGAT) activity.

Lecimibide (DuP 128) is a potent and specific acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor for antihyperlipidemia research.

F-1394 is an orally active acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor that inhibits dietary cholesterol absorption in mice. F-1394 can be used in cardiovascular disease research.

BAY 74-4113 is a DGAT1 inhibitor (IC₅₀: 72 nM). BAY 74-4113 can be used in obesity research.

(E)-Hyzetimibe ((E)-HS-25) (Compound I-1Z) is the trans isomer of Hyzetimibe (HY-107176A), a cholesterol-lowering agent. (E)-Hyzetimibe has cholesterol acyltransferase (ACTA) inhibitory activity, but its cholesterol-lowering effect is relatively weak. (E)-Hyzetimibe can inhibit the entry of hepatitis C virus (HCV) into host cells, and it has a synergistic effect when used in combination with interferon-α. (E)-Hyzetimibe can be used for the study of HCV infection.

ACAT-IN-9 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor extracted from patent EP1236468A1, example 207. ACAT-IN-9 inhibits NF-κB mediated transcription.

ACAT-IN-4 (Example 208) is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. ACAT-IN-4 inhibits NF-κB mediated transcription.

1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone, a quinolone alkaloid, is a diacylglycerol acyltransferase inhibitor and angiotensin II receptor blocker, with IC₅₀s of 20.1 μM and 34.1 μM, respectively. 1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone shows potent anti-Helicobacter pylori activity with the MIC of 10 μg/mL.

ACAT-IN-10 dihydrochloride is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor extracted from patent EP1236468A1, example 197. ACAT-IN-10 dihydrochloride weakly inhibits NF-κB mediated transcription.

CL-283796 is a potent and orally active acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor. CL-283796 reduces low-density lipoprotein (LDL) cholesterol without affecting cholesterol absorption in African green monkeys. CL-283796 can be used for hypercholesterolemia research.

Phenylpyropene C (S14-95), a JAK/STAT pathway inhibitor, can inhibit IFN-γ mediated expression of the reporter gene (IC₅₀=5.4~10.8 μM). Phenylpyropene C also is an inhibitor of acyl-CoA, with an IC₅₀ of 16.0 μM.

Bay-02752 (Bay o 2752) is a lipid-lowering agent. Bay-02752 inhibits acyl-CoA activity in liver microsomes (IC₅₀ = 0.95 μg/mL). Bay-02752 inhibits intestinal cholesterol absorption in rats. Bay-02752 inhibits gallstone formation in hamsters.

Teglicar chloride (ST1326 chloride) is an orally active, reversible, mixed-type, selective inhibitor of hepatic carnitine palmitoyltransferase I (L-CPT I), with an IC₅₀ of 1.1 μM against rat L-CPT I. Teglicar chloride reduces serum glucose levels. Teglicar chloride exhibits antiketotic activity in normal fasted rats. Teglicar chloride can be used in research related to type 2 diabetes and ketoacidosis.

ACAT-IN-6 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor extracted from patent EP1236468A1, example 200. ACAT-IN-6 potently inhibits NF-κB mediated transcription.