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Beschreibung

A cell-permeable, orally active, non-toxic bipiperidylcarboxamide derived compound that binds to the active site of acetyl-CoA carboxylase (ACC) at the interface between the two monomers of the CT dimer and acts as a potent, allosteric, and reversible, inhibitor of ACC (IC50 = 53 nM and 61 nM for rat liver ACC1 and ACC2). The inhibition is uncompetitive with respect to ATP and non-competitive with respect to acetyl-CoA, citrate, and bicarbonate. Shown to inhibit fatty acid synthesis in Sprague-Dawley rats, and in CD1 and ob/ob mice (ED50 = 13, 11, and 4 mg/kg). Stimulates fatty acid oxidation in CC12 cells in rat epitrochelearis muscle (ED50 = 57 nM) and reduces muscle malonyl-CoA levels. Improves insulin sensitivity in diet-induced obese animal models. Displays good metabolic stability and moderate pharmacokinetic properties (plasma half-life =1.5 h, Cmax = 345 ng/ml, and AUC = 960 ng/h/ml at 5 mg/kg i.v. or 10 mg/kg p.o.)., A cell-permeable, orally active, non-toxic bipiperidylcarboxamide derived compound that binds to the active site of acetyl-CoA carboxylase (ACC) at the interface between the two monomers of the CT dimer and acts as a potent, allosteric, and reversible, inhibitor of ACC (IC50 = 53 nM and 61 nM for rat liver ACC1 and ACC2). The inhibition is uncompetitive with respect to ATP and non-competitive with respect to acetyl-CoA, citrate, and bicarbonate. Shown to inhibit fatty acid synthesis in Sprague-Dawley rats, and in CD1 and ob/ob mice (ED50 = 13, 11, and 4 mg/kg). Stimulates fatty acid oxidation in CC12 cells in rat epitrochelearis muscle (ED50 = 57 nM) and reduces muscle malonyl-CoA levels. Improves insulin sensitivity in diet-induced obese animal models. Displays good metabolic stability and moderate pharmacokinetic properties (plasma half-life =1.5 h, Cmax = 345 ng/ml, and AUC = 960 ng/h/ml at 5 mg/kg i.v. or 10 mg/kg p.o.). Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water., ACC Inhibitor IV, CP-640186, is a cell-permeable, potent, allosteric, eversible inhibitor of ACC (IC₅,₀, = 53 and 61 nM for rat liver ACC1 & ACC2). The inhibition is uncompetitive with respect to ATP.