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    A922500
    A922500

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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 #: V0918
    CAS #: 959122-11-3Purity ≥98%

    Description: A922500 is a novel, highly potent, selective and orally bioactive  inhibitor for human and mouse Acyl CoA/diacylglycerol acyltransferase(DGAT-1) with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets. A 922500 confers weight loss and a reduction in liver triglycerides when dosed chronically in DIO mice and depletes serum triglycerides following a lipid challenge in a dose-dependent manner, thus, reproducing major phenotypical characteristics of DGAT-1(-/-) mice.

    References: J Pharmacol Exp Ther. 2009;330:526-31; J Med Chem. 2008;51:380-3; Eur J Pharmacol. 2010;637:155-61.

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    Molecular Weight (MW)428.48
    FormulaC26H24N2O4
    CAS No.959122-11-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 86 mg/mL (200.7 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)15% Captisol: 20mg/mL
    SynonymsA-922500; A922500; A 922500; 


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    In Vitro

    In vitro activity: A 922500 inhibits the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 with IC50 of 296 μM. A 922500 potently inhibits huDGAT-1 and mseDGAT-1.

    In VivoZucker fatty rats and diet-induced dyslipidemic hamsters are dosed orally with A 922500 (0.03, 0.3, and 3 mg/kg) for 14 days. Serum triglycerides ae significantly reduced by the 3 mg/kg dose of A 922500 in both the Zucker fatty rat (39%) and hyperlipidemic hamster (53%). These serum triglyceride changes are accompanied by significant reductions in free fatty acid levels by 32% in the Zucker fatty rat and 55% in the hyperlipidemic hamster. In addition, high-density lipoprotein-cholesterol is significantly increases (25%) in the Zucker fatty rat by A 922500 administered at 3 mg/kg. A 922500 confers weight loss and a reduction in liver triglycerides when dosed chronically in DIO mice and depletes serum triglycerides following a lipid challenge in a dose-dependent manner, thus, reproducing major phenotypical characteristics of DGAT-1(-/-) mice. A 922500 (0.03, 0.3 and 3 mg/kg, p.o.) dose-dependently attenuates the maximal postprandial rise in serum triglyceride concentrations.
    Animal modelMale Golden Syrian hamsters with hyperlipidemia, and Male Zucker fatty rats
    Formulation & DosageDissolved in Polyethylene glycol/hydroxypropyl-β-cyclodextrin (10% w/v); 0.03, 0.3, and 3 mg/kg; oral gavage
    References

    J Pharmacol Exp Ther. 2009 Aug;330(2):526-31; J Med Chem. 2008 Feb 14;51(3):380-3; Eur J Pharmacol. 2010 Jul 10;637(1-3):155-61.


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

    A922500

    Body weight (A), serum triglycerides (B), total cholesterol (C), LDL-cholesterol (D), HDL-cholesterol (E), and FFA (F) in hamsters on regular chow (normolipidemic) and after 2 weeks of a hyperlipidemic diet (dyslipidemic). J Pharmacol Exp Ther. 2009 Aug;330(2):526-31. 
     

    A922500

    Body weight (A), serum triglycerides (B), total cholesterol (C), LDL-cholesterol (D), HDL-cholesterol (E), LDL:HDL-cholesterol (F), and FFA (G) in hyperlipidemic hamsters before and after 14 days of treatment with vehicle or DGAT-1 inhibitor A-922500. J Pharmacol Exp Ther. 2009 Aug;330(2):526-31. 
     

    A922500

    Body weight (A), serum triglycerides (B), total cholesterol (C), LDL-cholesterol (D), HDL-cholesterol (E), and FFA (F) in Zucker rats before and after 14-days of treatment with vehicle or DGAT-1 inhibitor A-922500. J Pharmacol Exp Ther. 2009 Aug;330(2):526-31. 


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