CP-640186 is an isozyme-nonselective acetyl-CoA carboxylase (ACCase) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively with improved metabolic stability vs CP-610431.
CP-640186 is an orally active and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC50 values of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2, respectively. Acetyl-CoA carboxylase (ACC) serves as a pivotal enzyme in fatty acid metabolism, facilitating the synthesis of malonyl-CoA. CP-640186 additionally promotes muscle fatty acid oxidation [1][2].
CP-640186 (intravenous injection and oral gavage; Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg; once) exhibits lower drug exposure in rats compared to ob/ob mice at equivalent doses [1].
Treatment with CP-640186 (oral gavage; 100 mg/kg; once) results in a complete shift from carbohydrate utilization to fatty acid utilization as the primary source of energy at high exposure levels [1].
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