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    Avasimibe
    Avasimibe

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0803
    CAS #: 166518-60-1Purity ≥98%

    Description: Avasimibe (CI-1011; PD 148515; CI1011; CI 1011; PD148515; PD-148515) is a novel, potent and orally bioavailable inhibitor of acyl-Coenzyme A:cholesterol acyltransferase (ACAT) with the potential for the treatment of atherosclerosis and hyperlipidaemia. It inhibits ACAT1/2 with IC50s of 24 and 9.2 µM, respectively. It also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9 μM, 13.9 μM and 26.5 μM, respectively. 

    References: J Med Chem. 1996 Dec 20;39(26):5031-4; Atherosclerosis. 1998 Jan;136(1):79-87.

    Related CAS #: 166518-61-2 (sodium)  

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    Molecular Weight (MW)501.72
    FormulaC29H43NO4S
    CAS No.166518-60-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (199.3 mM)
    Water: <1 mg/mL
    Ethanol: 8 mg/mL (15.9 mM)
    Solubility (In vivo)2% DMSO+corn oil: 5mg/mL
    SynonymsCI1011; PD-148515; Avasimibe; PD 148515; CI-1011; CI 1011; PD148515; Avasimibe sodium.
    SMILES Codec1(C(C)C)cc(cc(c1CC(NS(Oc1c(cccc1C(C)C)C(C)C)(=O)=O)=O)C(C)C)C(C)C


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    In Vitro

    In vitro activity: Avasimibe is an acyl coenzyme A that inhibits ACAT with IC50 of 3.3 μM, it also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9 μM, 13.9 μM and 26.5 μM, respectively. Avasimibe can also reduce the synthesis and secretion of Apo B 100 in HepG2 cells. Avasimibe encapsulated in human serum albumin blocks cholesterol esterification for selective cancer treatment. Avasimibe could be an efficient therapy in the treatment of glioblastoma. 


    Kinase Assay: Avasimibe is an oral inhibitor of acyl-Coenzyme A:cholesterol acyltransferase (ACAT) with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively.


    Cell Assay: Avasimibe at concentration of 1μg/mL causes reduction of Total cholesterol (TC) and Esterified cholesterol (EC) through inhibiting LDL binding and decreasing scavenger receptor numbers during foam cell formation in human monocyte-derived macrophages (HMMs). Avasimibe at concentration of 2μg/mL enhances cholesterol efflux from established HMM foam cells preincubating with 10μg/ml LDL. Avasimibe inhibits Lipoprotein(a) accumulation in the culture media of primary monkey hepatocyte in a dose-dependent manner with 11.9% -31.3% inhibition, the change is mainly associated with decreased ApoA. Avasimibe incubating at concentration of 10 nM, 1 μM, and 10 μM for 24 hours in HepG2 cells reduce ApoB secretion into media by 25%, 27%, and 43%, respectively. Avasimibe decreases ApoB secretion by enhanced intracellular degradation of ApoB rather than decreased synthesis of ApoB. Avasimibe inhibits ACTC with IC50 of 3.3 μM in IC-21 macrophages with consideration of the total inhibitor concentration in the assay sample. Avasimibe inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9 μM, 13.9 μM and 26.5 μM, respectively. Avasimibe inhibits ACAT-1 expression and cholesterol ester synthesis in glioma cell lines. Avasimibe inhibits the growth of the glioma cells by inducing cell cycle arrest and apoptosis due to caspase-8 and caspase-3 activation.

    In VivoAvasimibe significantly reduces Lipoprotein(a) and total cholesterol levels in nine healthy male monkeys with a normal chow diet orally treated with CI-1011 at 30 mg/kg per day for 3 weeks, Lipoprotein(a) and total cholesterol levels reduce to 68 and 73% of control levels, respectively. Avasimibe decreases total cholesterol mainly due to reduction of low density lipoprotein (LDL). Avasimibe decreases amyloid plaque load in the cortex and hippocampus and reduces the levels of insoluble Abeta40 and Abeta42 and C-terminal fragments of amyloid precursor protein (APP) in brain extracts in young human APP transgenic mice. Avasimibe reduces diffuse amyloid plaques by suppression of astrogliosis and enhanced microglial activation in aged human APP transgenic mice.
    Animal modelMale cynomolgus monkeys
    Formulation & DosageDissolved in 0.9% sodium chloride solution; 30 mg/kg; p.o.
    ReferencesJ Med Chem. 1996 Dec 20;39(26):5031-4; Atherosclerosis. 1998 Jan;136(1):79-87.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Avasimibe

    Concentration-dependent induction of CY2C9 activity and immunoreactive protein by avasimibe in primary cultures of human hepatocytes. Drug Metab Dispos. 2004 Dec;32(12):1370-6. 
     

    Avasimibe

    Concentration-dependent induction of CYP1A1/2 activity by avasimibe in primary cultures of human hepatocytes. Drug Metab Dispos. 2004 Dec;32(12):1370-6. 
     

    Avasimibe

    Concentration-dependent induction of CY2B6 activity by avasimibe in primary cultures of human hepatocytes. Drug Metab Dispos. 2004 Dec;32(12):1370-6. 


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