欢迎光临源叶生物,登录 | 注册 |
当前位置: 首页 > 小分子抑制剂 > Metabolism > CP-640186 (hydrochloride)

浏览历史

S85888

CP-640186 (hydrochloride)

源叶(MedMol) 99%
  • 英文名:
  • CP-640186 (hydrochloride)
  • 别名:
  • CAS号:
  • 591778-70-0
  • 分子式:
  • C30H36ClN3O3
  • 分子量:
  • 522.0781
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S85888-5mg 99% ¥740.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S85888-10mg 99% ¥1190.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S85888-50mg 99% ¥3900.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S85888-100mg 99% ¥5600.00元 预计交期:2-3天 - - - EA 加入购物车
大包装询价

提交您的电话号码并同意《个人信息授权与保护申明》,到货后将短信提示。
提交

产品介绍

参考文献

质检证书(COA)

摩尔浓度计算器

相关产品

  • 提示:详情请下载说明书。
  • 产品描述: CP-640186 hydrochloride 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 hydrochloride can also stimulate muscle fatty acid oxidatio
  • 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 hours Result: 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、H2O
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 1.915 ml 9.577 ml 19.154 ml
    5 mM 0.383 ml 1.915 ml 3.831 ml
    10 mM 0.192 ml 0.958 ml 1.915 ml
    50 mM 0.038 ml 0.192 ml 0.383 ml
  • 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。
输入产品批号:

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:


质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)


  • =
    *
    *


源叶所有产品仅用作科学研究,销售产品行为均适用于我司网上所列通用销售条款。