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CP-610431

CAS No. : 591778-83-5

MCE 站：CP-610431

产品活性：CP-610431 是一种可逆的、ATP 非竞争性的、同工酶非选择性的乙酰辅酶 A 羧化酶 (ACC) 抑制剂。CP-610431 抑制 ACC1 和 ACC2，IC₅₀ 约为 50 nM。 CP-610431 可用于代谢综合征的研究。

研究领域：Metabolic Enzyme/Protease

作用靶点：Acetyl-CoA Carboxylase

In Vitro: CP-610431 is the active R-enantiomer of CP-497485. CP-610431 is more potent than the racemate CP-497485 in inhibiting rat ACC1 (IC₅₀=35.7 nM) ａnd ACC2 (IC₅₀=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.
CP-610431 inhibits fatty acid synthesis, triglyceride synthesis, TG secretion, ａnd apolipoprotein B secretion in HepG2 cells (ACC1) with EC₅₀s of 1.6, 1.8, 3.0, ａnd 5.7 μM, without affecting either cholesterol synthesis or apolipoprotein CIII secretion.
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) .
CP-610431 inhibits mouse primary hepatocyte fatty acid ａnd TG synthesis with IC₅₀ values of 0.11 ａnd 1.2 μM and inhibits TG secretion with an IC₅₀ of 10 μM.

In Vivo: CP-610431 inhibits fatty acid synthesis in CD1 mice ａnd ob/ob mice within 1 h after dose with ED₅₀s of 22 ａnd 4 mg/kg, respectively.

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