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CI-1011 (Avasimibe) | ACAT inhibitor

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Price:
$79.00
Catalog #:
C2410-10
Quantity:


Product Description

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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