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编 号：F759074
分子式：C30H37N3O2
分子量：471.63
分子式：C30H37N3O2
分子量：471.63
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CAS No: 591778-83-5
产品详情
生物活性：
CP-610431 is a reversible, ATP-uncompetitive, isozyme-nonselective acetyl-CoA carboxylase (ACC) inhibitor. CP-610431 inhibits ACC1 and ACC2 with IC50s of ~50 nM. CP-610431 can be used for the research of metabolic syndrome.
体内研究：
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.Animal Model:CD1 mice
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.
体外研究：
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.
CP-610431 is a reversible, ATP-uncompetitive, isozyme-nonselective acetyl-CoA carboxylase (ACC) inhibitor. CP-610431 inhibits ACC1 and ACC2 with IC50s of ~50 nM. CP-610431 can be used for the research of metabolic syndrome.
体内研究：
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.Animal Model:CD1 mice
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.
体外研究：
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.
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