| 货号 | 规格 | 价格 | 上海 | 北京 | 武汉 | 南京 | 购买数量 |
|---|---|---|---|---|---|---|---|
S88247-2mg |
98.80% | ￥408.00 | 7 | - | - | - |
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S88247-5mg |
98.80% | ￥670.00 | 5 | - | - | - |
|
S88247-10mg |
98.80% | ￥1080.00 | 7 | - | - | - |
|
S88247-25mg |
98.80% | ￥2250.00 | 6 | - | - | - |
|
S88247-50mg |
≥98% | ￥3200.00 | 货期：2-3天 | - | - | - |
|
S88247-100mg |
≥98% | ￥5600.00 | 货期：2-3天 | - | - | - |
|
| 产品描述： | CP-640186 is an orally active and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively. Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty acid metabolism that enables the synthesis of malonyl-CoA. CP-640186 can also stimulate muscle fatty acid oxidation | ||||||||||||||||||||
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| 靶点： | IC50: 53 nM (rat liver ACC1) and 61 nM (rat skeletal muscle ACC2);Acetyl-CoACarboxylase | ||||||||||||||||||||
| 体外研究： | CP-640186 (20 µM; 48 h) treatment can inhibit H460 cell growth. CP-640186 (0.1 nM-100 µM; 2 h) treatment increases fatty acid metabolism in a concentration-dependent manner in C2C12 cells and muscle strips. CP-640186 (0.62-1.8 µM; 2 h) treatment inhibits fatty acid synthesis and TG synthesis in HepG2 cells. Cell Proliferation Assay Cell Line: Human fibroblasts and H460 cells Concentration: 20 µM Incubation Time: 48 hours Result: Led to a ∼30% decrease in cell number compared to vehicle-treated controls. Cell Viability Assay Cell Line: C2C12 cells and muscle strips Concentration: 0.1 nM-100 µM Incubation Time: 2 hourResult: Stimulated palmitate acid oxidation with an EC50 of 57 nM and a maximal stimulation of 280% in C2C12 cells.Stimulated palmitate acid oxidation with an EC50 of 1.3 μM and a maximal stimulation of 240% in isolated rat epitrochlearis muscle. Cell Viability Assay Cell Line: HepG2 cells Concentration: 0.62-1.8 µM Incubation Time: 6 hours Result: Inhibited fatty acid synthesis and TG synthesis in HepG2 cells with EC50s of 0.62 μM and 1.8 μM, respecticely. | ||||||||||||||||||||
| 体内研究： | CP-640186 (oral gavage; 4.6-21 mg/kg; once) demonstrates acute efficacy. CP-640186 (intravenous injection and oral gavage; Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg; once) shows lowe drug exposure in the rat than the ob/ob mouse at equal doses. CP-640186 (oral gavage; 100 mg/kg; once) treatment shows a complete shift from carbohydrate utilization to fatty acid utilization as a source of energy at high exposure level. Animal Model: Male ob/ob mice Dosage: 4.6-21 mg/kg Administration: Oral gavage; 4.6-21 mg/kg; once Result: Demonstrated acute efficacy for up to 8 h after oral administration, exhibiting ED50 values of 4.6, 9.7, and 21 mg/kg, at 1, 4, and 8 h, respectively, after treatment. Animal Model: Male Sprague-Dawley rats Dosage: Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg Administration: Intravenous injection and oral gavage; Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg; once Result: Showed a plasma half-life of 1.5 h, a bioavailability of 39%, a Clp of 65 ml/min/kg, a Vdss of 5 liters/kg, an oral Tmax of 1.0 h, an oral Cmax of 345 ng/mL, and an oral AUC0-∞ of 960 ng•h/mL. Animal Model: Male ob/ob mice Dosage: Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg Administration: Intravenous injection and oral gavage; Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg; once Result: Showed a plasma half-life of 1.1 h, a bioavailability of 50%, a Clp of 54 ml/min/kg, an oral Tmax of 0.25 h, an oral Cmax of 2177 ng/mL, and an oral AUC0-∞ of 3068 ng•h/mL. Animal Model: Twenty male Sprag | ||||||||||||||||||||
| 参考文献： | 1. Harwood HJ Jr, et al. Isozyme-nonselective N-substituted bipiperidylcarboxamide acetyl-CoA carboxylase inhibitors reduce tissue malonyl-CoA concentrations, inhibit fatty acid synthesis, and increase fatty acid oxidation in cultured cells and in experimental animals. J Biol Chem. 2003 Sep 26;278(39):37099-111. 2. Yamashita T, et al. Design, synthesis, and structure-activity relationships of spirolactones bearing 2-ureidobenzothiophene as acetyl-CoA carboxylases inhibitors. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6314-8. 3. Daniel Hess, et al. Inhibition of stearoylCoA desaturase activity blocks cell cycle progression and induces programmed cell death in lung cancer cells. PLoS One. 2010 Jun 30;5(6):e11394. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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