Synonyms: (3R)-Anthracen-9-yl-[3-(morpholine-4-carbonyl)-[1,4']bipiperidinyl-1'-yl]-methanone hydrochloride; CP 640186 hydrochloride; CP640186 hydrochloride; [(3R)-1'-(9-Anthracenylcarbonyl)[1,4'-bipiperidin]-3-yl]-4-morpholinyl-methanone hydrochloride
Molecular Formula: C30H35N3O3 · HCl
Molecular Weight: 522.08
Linear Structural Formula: C30H35N3O3 · HCl
MDL Number: MFCD28167776
Purity: >=95% (HPLC)
Storage: room temp
Biochem Physiol Actions: CP-640186 is a potent and orally active acetyl-CoA carboxylase 1/2 (ACC-alpha/beta, ACC1/2) inhibitor (IC50 ~50 nM) that 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 muM, respectively), but not cholesterol synthesis or apoC3 secretion in HepG2 cells (ACC1), as well as stimulates FA oxidation in C2C12 cells (ACC2) and in rat epitrochlearis muscle strips (EC50 = 57 nM and 1.3 muM, 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 rat whole body FA oxidation (ED50 >=30 mg/kg) in vivo.
Legal Information: Sold for research purposes under agreement from Pfizer Inc.