CP-640186 hydrochloride
目录号: PL04394 纯度: ≥99%
CAS No. :591778-70-0
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中文名称
CP-640186 hydrochloride
中文别名
盐酸CP-640186
英文名称
CP-640186 hydrochloride
英文别名
CP-640186 (hydrochloride);CP640186 hydrochloride;(3R)-Anthracen-9-yl-[3-(morpholine-4-carbonyl)-[1,4′]bipiperidinyl-1′-yl]-methanone hydrochloride;[(3R)-1′-(9-Anthracenylcarbonyl)[1,4′-bipiperidin]-3-yl]-4-morpholinyl-methanone hydrochloride;CP640186;(R)-anthracen-9-yl(3-(morpholine-4-carbonyl)-[1,4'-bipiperidin]-1'-yl)methanone;04L1E4J3ZT;CP 640186;(3R)-1'-(9-anthrylcarbonyl)-3-(morpholin-4-ylcarbonyl)-1,4'-bipiperidine;(3R)-1'-(anthracen-9-ylcarbonyl)-3-(morpholin-4-ylcarbonyl)-1,4'-bipiperidine;RCP;{(3R)-1'-(anthracen-9-ylcarbonyl)[1,4'-bipiperidin]-3-yl}(morpholin-4-yl)methanone;[(3R)-1-[1-(anthracene-9-carbonyl)piperidin-4-yl]piperidin-3-yl]-morpholin-;CP-640186 hydrochloride
Cas No.
591778-70-0
分子式
C30H35N3O3
分子量
485.62
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
CP-640186 hydrochloride 是一种具有口服活性的、可透过细胞的乙酰-CoA 羧化酶 (ACC) 抑制剂,其对大鼠肝脏 ACC1 和大鼠骨骼肌 ACC2 的 IC50s 分别为 53 nM 和 61 nM。乙酰-CoA羧化酶 (ACC) 是脂肪酸代谢的一个关键酶,能够合成丙二酰-CoA。CP-640186 hydrochloride 还可以刺激肌肉脂肪酸的氧化。
生物活性
CP-640186 hydrochloride is an orally active and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC 50 s 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 oxidation.
性状
Solid
IC50 & Target[1][2]
IC50: 53 nM (rat liver ACC1) and 61 nM (rat skeletal muscle ACC2)
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 experiment
[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.
溶解度数据
In Vitro: H2O : 50 mg/mL (95.77 mM; Need ultrasonic)DMSO : ≥ 48 mg/mL (91.94 mM)
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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