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CP-640186 hydrochloride
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。
CP-640186 hydrochloride图片
CAS NO:591778-70-0
包装与价格：
包装价格(元)
10 mM * 1 mL in DMSO电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

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-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 Clpof 65 ml/min/kg, a Vdssof 5 liters/kg, an oral Tmaxof 1.0 h, an oral Cmaxof 345 ng/mL, and an oral AUC0-∞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 Clpof 54 ml/min/kg, an oral Tmaxof 0.25 h, an oral Cmaxof 2177 ng/mL, and an oral AUC0-∞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 mg5 mg10 mg
1 mM1.9154 mL9.5771 mL19.1542 mL
5 mM0.3831 mL1.9154 mL3.8308 mL
10 mM0.1915 mL0.9577 mL1.9154 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。