CP-640186 hydrochloride

Name: CP-640186 hydrochloride
Brand: MedChemExpress
SKU: HY-15259A
Rating: 5.0 (8 reviews)

Cat. No.: HY-15259A Purity: 99.90%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

CP-640186 hydrochloride Chemical Structure

CAS No. : 591778-70-0

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 103	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 103	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 144	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 480	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 768	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of CP-640186 hydrochloride:

CP-640186 Get quote

8 Publications Citing Use of MCE CP-640186 hydrochloride

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

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

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 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^[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.

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 the ob/ob mouse 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male ob/ob mice^[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 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^[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_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^[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_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^[1]
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%.

Molecular Weight

522.08

Formula

C₃₀H₃₆ClN₃O₃

CAS No.

591778-70-0

Appearance

Solid

Color

Light yellow to pink

SMILES

O=C([C@H]1CN(C2CCN(C(C3=C(C=CC=C4)C4=CC5=C3C=CC=C5)=O)CC2)CCC1)N6CCOCC6.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

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

DMSO : ≥ 48 mg/mL (91.94 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 100 mg/mL (191.54 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.90%

Select Batch:

Data Sheet (285 KB) SDS (393 KB)

COA (252 KB) LCMS (265 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	1.9154 mL	9.5771 mL	19.1542 mL	47.8854 mL
	5 mM	0.3831 mL	1.9154 mL	3.8308 mL	9.5771 mL
	10 mM	0.1915 mL	0.9577 mL	1.9154 mL	4.7885 mL
	15 mM	0.1277 mL	0.6385 mL	1.2769 mL	3.1924 mL
	20 mM	0.0958 mL	0.4789 mL	0.9577 mL	2.3943 mL
	25 mM	0.0766 mL	0.3831 mL	0.7662 mL	1.9154 mL
	30 mM	0.0638 mL	0.3192 mL	0.6385 mL	1.5962 mL
	40 mM	0.0479 mL	0.2394 mL	0.4789 mL	1.1971 mL
	50 mM	0.0383 mL	0.1915 mL	0.3831 mL	0.9577 mL
	60 mM	0.0319 mL	0.1596 mL	0.3192 mL	0.7981 mL
	80 mM	0.0239 mL	0.1197 mL	0.2394 mL	0.5986 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.