Loading... Please wait...

Our Newsletter


CI-1011 (Avasimibe) | ACAT inhibitor

  • CI-1011 (Avasimibe).jpg
  • CI-1011 (Avasimibe), 400x400px, png
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.

Write your own product review

Product Reviews

This product hasn't received any reviews yet. Be the first to review this product!

Add to Wish List

Click the button below to add the CI-1011 (Avasimibe) | ACAT inhibitor to your wish list.

You Recently Viewed...