Bulk Inquiry
Avasimibe
- CI-1011
- Soluble in DMSO
- MF: C29H43NO4S
- MW: 501.72
Description
Avasimibe (CI-1011) is an orally active inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT/SOAT) with IC50 values of 24 μM and 9.2 μM for ACAT1 (SOAT1) and ACAT2 (SOAT2), respectively. By inhibiting intracellular cholesterol esterification, Avasimibe modulates lipid metabolism and cholesterol homeostasis in multiple cell types.
ACAT enzymes catalyze the conversion of free cholesterol into cholesteryl esters for intracellular storage and play central roles in lipid metabolism, macrophage foam cell formation, atherosclerosis, cancer metabolism, and immune cell function. Avasimibe has been widely used to investigate cholesterol ester metabolism and has demonstrated therapeutic potential in models of cardiovascular disease, cancer, and immuno-oncology. Inhibition of ACAT1 has also been shown to enhance T-cell function and antitumor immunity, making Avasimibe a valuable chemical tool for studying cholesterol metabolism, immune regulation, and metabolic reprogramming.
Key Features
- Orally active ACAT/SOAT inhibitor
- IC50: 24 μM (ACAT1/SOAT1) and 9.2 μM (ACAT2/SOAT2)
- Inhibits intracellular cholesterol esterification
- Modulates cellular lipid metabolism and cholesterol homeostasis
- Widely used tool for metabolism, cardiovascular, and cancer research
Applications
- Cholesterol metabolism and lipid biology research
- ACAT1 and ACAT2 signaling studies
- Atherosclerosis and foam cell formation investigations
- Cancer metabolism and immuno-oncology research
- T-cell biology and metabolic regulation studies
More Information
| Parent CAS No. | 166518-60-1 |
|---|---|
| Chemical Name | N-2,6-Diisopropylphenoxysulfonyl(2,4,6-triisopropylphenyl)acetamide |
| SMILES | O(S(NC(=O)CC1C(C(C)C)=CC(C(C)C)=CC=1C(C)C)(=O)=O)C1=C(C=CC=C1C(C)C)C(C)C |
| MFCD | MFCD00934956 |
| InChi | InChI=1S/C29H43NO4S/c1-17(2)22-14-25(20(7)8)27(26(15-22)21(9)10)16-28(31)30-35(32,33)34-29-23(18(3)4)12-11-13-24(29)19(5)6/h11-15,17-21H,16H2,1-10H3,(H,30,31) |
| InChiKey | PTQXTEKSNBVPQJ-UHFFFAOYSA-N |
| CID | 166558 |
| Short Description | ACAT inhibitor |
References
- HT Lee et al. Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets. J Med Chem. 1996 Dec 20;39(26):5031-4.
- T Ohshiro et al. Pyripyropene A, an acyl-coenzyme A:cholesterol acyltransferase 2-selective inhibitor, attenuates hypercholesterolemia and atherosclerosis in murine models of hyperlipidemia. Arterioscler Thromb Vasc Biol. 2011 May;31(5):1108-15.
