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。
| 生物活性 | CP-610431 is a reversible, ATP-uncompetitive, isozyme-nonselectiveacetyl-CoA carboxylase(ACC) inhibitor. CP-610431 inhibitsACC1andACC2withIC50s of ~50 nM. CP-610431 can be used for the research of metabolic syndrome[1]. |
体外研究
(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[1].
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[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 IC50 values of 0.11 and 1.2 μM and inhibits TG secretion with an IC50 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 IC50 of 1.6 μM, TG synthesis with an IC50 of 1.8 μM, TG secretion with an IC50 of 3.0 μM, and apoB secretion with an IC50 of 5.7 μM. |
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体内研究
(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[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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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