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CP-640186

目录号: PC16780 纯度: ≥98%

乙酰辅酶A羧化酶（ACCase）抑制剂。CP-640186是乙酰辅酶A羧化酶（ACCase）抑制剂，对鼠肝ACCase1和骨骼肌ACCase2的IC50s分别为53 nM和61 nM，比CP-610431有更好的代谢稳定性。

CAS No. :591778-68-6

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中文名称

CP-640186

中文别名

CP640186 抑制剂

英文名称

CP-640186

英文别名

[(3R)-1-[1-(anthracene-9-carbonyl)piperidin-4-yl]piperidin-3-yl]-morpholin-4-ylmethanone;(R)-ANTHRACEN-9-YL(3-(MORPHOLINE-4-CARBONYL)-1,4'-BIPIPERIDIN-1'-YL)METHANONE.HCL;Cp 640186;CP640186 HCl;(Anthracen-9-yl)[(3R)-3-[(morpholin-4-yl)carbonyl][1,4']bipiperidinyl-1'-yl]methanone;CP-640186;(3R)-1'-(9-anthrylcarbonyl)-3-(morpholin-4-ylcarbonyl)-1,4'-bipiperidine;CP640186;(R)-anthracen-9-yl(3-(morpholine-4-carbonyl)-[1,4'-bipiperidin]-1'-yl)methanone;04L1E4J3ZT;(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

Cas No.

591778-68-6

分子式

C₃₀H₃₅N₃O₃

分子量

485.62

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

详情描述

生物活性

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.

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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(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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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 Cl_p of 65 ml/min/kg, a V_dss of 5 liters/kg, an oral T_max of 1.0 h, an oral C_max of 345 ng/mL, and an oral AUC_0-∞ 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 Cl_p of 54 ml/min/kg, an oral T_max of 0.25 h, an oral C_max of 2177 ng/mL, and an oral AUC_0-∞ of 3068 ng?h/mL.

Animal Model:	Twenty male Sprague-Dawley rats (350-400 g) fasted and then refed a high sucrose diet for 2 days; additional eight rats fasted for 24 h
Dosage:	100 mg/kg
Administration:	Oral gavage; 100 mg/kg; once
Result:	Resulted in time-dependent reductions in RQ (a ratio of CO₂ production to O₂ consumption) of up to 64%.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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 [Information]

[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. [Information]

[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. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (205.92 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0592 mL	10.2961 mL	20.5922 mL
5 mM	0.4118 mL	2.0592 mL	4.1184 mL
10 mM	0.2059 mL	1.0296 mL	2.0592 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.15 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.15 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.15 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.15 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.15 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.15 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

搜索质检报告(COA)

产品使用指南

Data Sheet

[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 [Information]

[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. [Information]

[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. [Information]

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。

CP-640186

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