CI-1011 (Avasimibe) is an orally-available acylsulfamic acid inhibitor of Acyl Coenzyme A cholesterol acyltransferase (ACAT), an enzyme that catalyzes the esterification of cholesterol. inhibition of ACAT by CI-1011 presumably operates by modulating apoB synthesis and secretion, thereby lowering plasma concentration of apoB-containing lipoproteins. [3] CI-1011 inhibits ACAT at 3.3 uM, though it has been shown to be more potent dependent on microsome concentration. [1] CI-1011 also inhibits CYP450 enzymes 2C9, 1A2, and 2C19 at 2.9 uM, 13.9 uM, and 26.5 uM, respectively. [2] CI-1011 has been shown to be a PXR activator and has CYP3A4 induction profile approximately 10 fold more potent than rifampin. [2]CI-1011 reduces plasma triglyceride levels in chow-fed rats, cholesterol-fed rats, sucrose-fed rats, and hamsters. [1] In addition to inhibiting lipid accumulation in macrophages, and thus reducing atherosclerotic lesion occurrence, CI-1011 also has plaque-stabilizing properties by inhibiting MMP expression and activity.
Technical information:
| Chemical Formula: | C29H43NO4S | |
| CAS #: | 166518-60-1 | |
| Molecular Weight: | 501.72 | |
| Purity: | > 98% | |
| Appearance: | White | |
| Chemical Name: | 2,6-diisopropylphenyl 2-(2,4,6-triisopropylphenyl)acetylsulfamate | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | CI-1011, CI1011, Avasimibe, PD-148515, PD148515 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Llaverias et al., Pharmacology of the ACAT inhibitor avasimibe (CI-1011). Cardiovascular Drug Rev. 2006, 21(1), 33-50. Pubmed ID:12595916 |
| 2. | Sahi et al., Effects of avasimibe on cytochrome P450 2C9 expression in vitro and in vivo. Drug Metabolism and Disposition, 2004, 32(12), 1370-1376. Pubmed ID:15333513 |
| 3. | Burnett et al., Inhibition of ACAT by avasimibe decreases both VLDL and LDL apolipoprotein B production in miniature pigs. J. Lipid Res. 1999, 40, 1317-1327. Pubmed ID:10393217 |
Other Information:
Product Specification (pdf) MSDS (pdf) Certificate of Analysis is available upon request.
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