CP-610431 T40675

Product Introduction
Bioactivity


英文名: CP-610431

描述: CP-610431 is a reversible, ATP-uncompetitive inhibitor of acetyl-CoA carboxylase (ACC), exhibiting isozyme nonselectivity. It inhibits both ACC1 and ACC2 with IC50 values of approximately 50 nM. CP-610431 offers potential application in metabolic syndrome research.

体外活性: CP-610431 is the active R-enantiomer of CP-497485. CP-610431 is more potent than the racemate CP-497485 in inhibiting rat ACC1 (IC 50 =35.7 nM) and ACC2 (IC 50 =55 nM), whereas the?S-enantiomer, CP-610432, does not substantially inhibit either ACC isoform at concentrations of up to 3 μM. CP-610431 is more potent than CP-497485 in inhibiting HepG2 cell fatty acid and triglyceride (TG) synthesis and in inhibiting TG and apoB secretion[1]. CP-610431 inhibits fatty acid synthesis, triglyceride synthesis, TG secretion, and apolipoprotein B secretion in HepG2 cells (ACC1) with EC 50 s of 1.6, 1.8, 3.0, and 5.7 μM, without affecting either cholesterol synthesis or apolipoprotein CIII secretion[1]. CP-610431 inhibits both liver and skeletal muscle ACC activity from all three species with essentially equal potency (rat, 36?versus?55 nM; mouse, 50?versus?63 nM; cynomolgus macaque, 70?versus?26 nM)[1]. CP-610431 inhibits mouse primary hepatocyte fatty acid and TG synthesis with IC 50 values of 0.11 and 1.2 μM?and inhibits TG secretion with an IC 50 of 10 μM[1]. Cell Viability Assay[1]Cell Line: HepG2 cells Concentration: 0.1, 1, 10 μM Incubation Time: 24 hours Result: Dose-dependently inhibited HepG2 cell fatty acid synthesis with an IC 50 of 1.6 μM, TG synthesis with an IC 50 of 1.8 μM, TG secretion with an IC 50 of 3.0 μM, and apoB secretion with an IC 50 of 5.7 μM.

体内活性: CP-610431 inhibits fatty acid synthesis in CD1 mice and ob/ob mice within 1 h after dose with ED 50 s of 22 and 4 mg/kg,?respectively[1]. Animal Model: CD1 mice[1]Dosage: 30 and 100 mg/kg for fasting CD1 mice; 10, 30, and 100 mg/kg for non-fasting CD1 mice Administration: Intraperitoneal administration; 1 hour Result: Inhibited hepatic fatty acid synthesis in fasting CD1 mice by 64±12%, and 77±4% at doses of 30 and 100 mg/kg, respectively. Inhibited hepatic fatty acid synthesis in non-fasting CD1 mice by 18%, 51%, and 75% at doses of 10, 30 and 100 mg/kg, respectively.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: CP 610431 | CP610431 | CP-610431

CP-610431 T40675信息由TargetMol中国为您提供，如您想了解更多关于CP-610431 T40675报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途