CP-640186 hydrochloride|cas:591778-70-0|西域试剂

CP-640186 hydrochloride,99.90%

产品编号：Bellancom-15259A| CAS NO：591778-70-0| 分子式：C₃₀H₃₆ClN₃O₃| 分子量：522.08

CP-640186 hydrochloride是一种有效且可透过细胞的乙酰辅酶A羧化酶 (ACC)抑制剂，抑制大鼠肝脏ACC1和大鼠骨骼肌ACC2的 IC50为53 nM和61 nM。

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-15259A	￥800.00	杭州北京（现货）
Bellancom-15259A	￥1200.00	杭州北京（现货）
Bellancom-15259A	￥1950.00	杭州北京（现货）
Bellancom-15259A	￥6800.00	杭州北京（现货）
Bellancom-15259A	￥10500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

CP-640186 hydrochloride

产品介绍

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 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 oxidation.

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.

西域 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.

西域 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%.

体内研究

西域 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%.

体内研究

西域 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%.

性状

Solid

溶解性数据

In Vitro:

H₂O : 50 mg/mL (95.77 mM; Need ultrasonic)

DMSO : ≥ 48 mg/mL (91.94 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9154 mL	9.5771 mL	19.1542 mL
5 mM	0.3831 mL	1.9154 mL	3.8308 mL
10 mM	0.1915 mL	0.9577 mL	1.9154 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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 (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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.

请依序添加每种溶剂： PBS
Solubility: 100 mg/mL (191.54 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.79 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.79 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 ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.79 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.79 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
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.79 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.79 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。

*以上所有助溶剂都可在西域网站选购。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献

. 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 [Content Brief]

. 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. [Content Brief]

. 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. [Content Brief]

化学品安全说明书(MSDS)

下载MSDS

质检证书(COA)

产品编号(Item Number)

批号(Lot Number)

1. 物质的识别

产品名：	CP-640186 HCl
CAS号：	591778-70-0
制造商/供应商：	西域试剂网站：www.hzbp.cn 邮件：13911702513@139.com

2. 合成/成分数据

产品名：	CP-640186 HCl
分子式：	C30H36ClN3O3
分子量：	522.08

3. 急救措施

吸入后：	如果吸入，移至空气新鲜处，如果呼吸困难，给输氧，如呼吸停止，给予人工呼吸。
皮肤接触后：	用大量的水冲洗，移除污染的衣服和鞋子。
眼睛接触后：	检查并取下隐形眼镜，并用大量的水冲洗；呼叫医生。
吞食后：	如果吞食，用大量纯净水漱口；呼叫医生。

4. 消防措施

适当的灭火剂：	雾状水，二氧化碳，干粉或泡沫。
防护设备：	穿戴自给式呼吸器和防护服，以防止与皮肤和眼睛接触。

5. 泄漏应急处理

安全防范措施：	封锁泄漏区域；穿戴自给式呼吸器，防护服和厚橡胶手套。
清洁/收集措施：	使用液体粘合原料（硅藻土，通用粘合剂）吸取精细粉末；使用酒精擦洗表面和设备除去污渍；根据第11条处理被污染的材料。

6. 处理和储存

安全处理说明：	避免吸入和接触皮肤，眼睛及衣物；材料可能略微具有刺激性。
储存：	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月

7. 接触控制和个人防护

呼吸设备：	NIOSH / MSHA认可的呼吸器。
双手保护：	耐化学腐蚀的橡胶手套。
眼睛防护：	化学安全护目镜。

8. 稳定性和反应活性

稳定性：	按照说明存储是稳定的；避免强氧化剂。
热分解/其他要避免的情况：	避免光和热。

9. 毒性资料

急性毒性：	无可用资料。
主要刺激性影响：	无可用资料。
在皮肤上：	无可用资料。
对眼睛：	无可用资料；可能具有刺激性。

10. 生态资料

一般注意事项：

无可用资料。

11. 废弃处置

按照所在国家，省份，县市和地方的法规处置。

12. 运输信息

正确的运输名称：	无
非危险品运输：	这种物质被视为非危险品运输。

13. 法规信息

尚未有针对此产品作出的化学安全性评估。

14. 其他信息

[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.

CP-640186 hydrochloride,99.90%

CP-640186 hydrochloride

化学品安全说明书(MSDS)

质检证书(COA)

1. 物质的识别

2. 合成/成分数据

3. 急救措施

4. 消防措施

5. 泄漏应急处理

6. 处理和储存

7. 接触控制和个人防护

8. 稳定性和反应活性

9. 毒性资料

10. 生态资料

11. 废弃处置

12. 运输信息

13. 法规信息

14. 其他信息

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