CP-640186 hydrochloride

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

591778-70-0

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-permeableAcetyl-CoA carboxylase(ACC) inhibitor withIC₅₀s 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^[1]^[2].

IC₅₀& Target

IC50: 53 nM (rat liver ACC1) and 61 nM (rat skeletal muscle ACC2)^[1]

体外研究
(In Vitro)

CP-640186 (20 μM; 48 h) treatment can inhibit H460 cell growth^[3].
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^[1].
CP-640186 (0.62-1.8 μM; 2 h) treatment inhibits fatty acid synthesis and TG synthesis in HepG2 cells^[1].

Cell Proliferation Assay^[3]

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^[1]

Cell Line:	C2C12 cells and muscle strips
Concentration:	0.1 nM-100 μM
Incubation Time:	2 hours
Result:	Stimulated palmitate acid oxidation with an EC₅₀of 57 nM and a maximal stimulation of 280% in C2C12 cells. Stimulated palmitate acid oxidation with an EC₅₀of 1.3 μM and a maximal stimulation of 240% in isolated rat epitrochlearis muscle.

Cell Viability Assay^[1]

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^[1].
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 theob/obmouse at equal doses^[1].
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^[1].

Animal Model:	Maleob/obmice^[1]
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 ED₅₀values of 4.6, 9.7, and 21 mg/kg, at 1, 4, and 8 h, respectively, after treatment.

Animal Model:	Male Sprague-Dawley rats^[1]
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_pof 65 ml/min/kg, a V_dssof 5 liters/kg, an oral T_maxof 1.0 h, an oral C_maxof 345 ng/mL, and an oral AUC_0-∞of 960 ngoh/mL.

Animal Model:	Maleob/obmice^[1]
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_pof 54 ml/min/kg, an oral T_maxof 0.25 h, an oral C_maxof 2177 ng/mL, and an oral AUC_0-∞of 3068 ngoh/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^[1]
Dosage:	100 mg/kg
Administration:	Oral gavage; 100 mg/kg; once
Result:	Resulted in time-dependent reductions in RQ (a ratio of CO₂production to O₂consumption) of up to 64%.

分子量

522.08

性状

Solid

Formula

C₃₀H₃₆ClN₃O₃

CAS 号

591778-70-0

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)

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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-CDin 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 μL20% 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本网站选购。