An ACAT inhibitor
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Avasimibe

Item No. 18129

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2,6-bis(1-methylethyl)phenyl ester N-[2-[2,4,6-tris(1-methylethyl)phenyl]acetyl]-sulfamic acid
CAS Number
166518-60-1
Synonyms
  • Cl-1011
  • PD-148515
Molecular Formula
C29H43NO4S
Formula Weight
501.7
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 10 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.25 mg/mlEthanol: 2 mg/ml
SMILES
CC(C)C1=C(OS(NC(CC2=C(C(C)C)C=C(C(C)C)C=C2C(C)C)=O)(=O)=O)C(C(C)C)=CC=C1
InChi Code
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)
InChi Key
PTQXTEKSNBVPQJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $54

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    10 mg

    $85

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    25 mg

    $185

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    50 mg

    $315

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    Product Description

    Acyl-Coenzyme A:cholesterol acyltransferases (ACAT1 and ACAT2) catalyze the formation of cholesterol esters from cholesterol and long chain fatty acyl-coenzyme A, and may play a role in the development of atherosclerosis.1 Avasimibe is an orally bioavailable inhibitor of ACAT (IC50s = 24 and 9.2 µM for ACAT1 and ACAT2, respectively).2 It reduces foam cell formation in human macrophages in vitro, enhancing free cholesterol efflux and inhibiting the uptake of modified LDL and dose-dependently reduces plasma total triglyceride and VLDL cholesterol levels in cholesterol-fed animal models.3,4 Avasimibe inhibition of ACAT has been used to decrease amyloid β generation in models of Alzheimer’s disease.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Buhman, K.F., Accad, M., and Farese, R.V., Jr. Mammalian acyl-CoA:cholesterol acyltransferases. Biochim. Biophys. Acta 1529(1-3), 142-154 (2000).

    2. Ohshiro, T., Matsuda, D., Sakai, K., 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. 31(5), 1108-1115 (2011).

    3. Llaverías, G., Laguna, J.C., and Alegret, M. Pharmacology of the ACAT inhibitor avasimibe (CI-1011). Cardiovasc. Drug Rev. 21(1), 33-50 (2003).

    4. Burnett, J.R., Wilcox, L.J., Telford, D.E., et al. Inhibition of ACAT by avasimibe decreases both VLDL and LDL apolipoprotein B production in miniature pigs. J. Lipid Res. 40(7), 1317-1327 (1999).

    5. Huttunen, H.J., Peach, C., Bhattacharyya, R., et al. Inhibition of acyl-coenzyme A: cholesterol acyl transferase modulates amyloid precursor protein trafficking in the early secretory pathway. The FASEB Journal 23(11), 3819-3828 (2009).