CP-640186 (hydrochloride) Chemical Properties

storage temp. 

Store at -20°C

solubility 

DMSO:39.0(Max Conc. mg/mL);74.7(Max Conc. mM)
H2O:50.0(Max Conc. mg/mL);95.77(Max Conc. mM)

form 

Solid

color 

Light yellow to pink

Water Solubility 

H2O: 2mg/mL, clear (warmed)

CP-640186 (hydrochloride) Usage And Synthesis

Uses

CP 640186 Hydrochloride can be used as acetyl CoA carboxylase inhibitors against metabolic syndrome and other disorders.

Biological Activity

CP-640186 is a potent and orally active acetyl-CoA carboxylase 1/2 (ACC-alpha/beta, ACC1/2) inhibitor (IC50 ~50 nM) th at targets the carboxyltransferase (CT) domain at the ACC dimer interface (via tight interactions with the putative biotin-binding site) in a reversible manner, uncompetitive with respect to ATP, and non-competitive with respect to bicarbonate, acetyl-CoA, and citrate. CP-610431 inhibits fatty acid (FA) synthesis, triglyceride (TG) synthesis, TG and apoB secretion (IC50 = 1.6, 1.8, 3.0, and 5.7 μM, respectively), but not cholesterol synthesis or apoC3 secretion in HepG2 cells (ACC1), as well as stimulates FA oxidation in C2C12 cells (ACC2) and in r at epitrochlearis muscle strips (EC50 = 57 nM and 1.3 μM, respectively). Oral administration is shown to inhibit FA synthesis in rats, CD1 mice, and ob/ob mice (ED50 = 13, 11, and 4 mg/kg, respectively) and stimulate r at whole body FA oxidation (ED50 ∼30 mg/kg) in vivo.

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