1. Metabolic Enzyme/Protease
  2. Acetyl-CoA Carboxylase
  3. CP-640186 hydrochloride

CP-640186 hydrochloride 

Cat. No.: HY-15259A Purity: 99.90%
COA Handling Instructions

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

CP-640186 hydrochloride Chemical Structure

CAS No. : 591778-70-0

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 138 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 138 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 192 In-stock
Estimated Time of Arrival: December 31
50 mg USD 660 In-stock
Estimated Time of Arrival: December 31
100 mg USD 900 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of CP-640186 hydrochloride:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

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].

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].

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 Clp of 65 ml/min/kg, a Vdss of 5 liters/kg, an oral Tmax of 1.0 h, an oral Cmax of 345 ng/mL, and an oral AUC0-∞ 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 Clp of 54 ml/min/kg, an oral Tmax of 0.25 h, an oral Cmax of 2177 ng/mL, and an oral AUC0-∞ 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.
SMILES

O=C([[email protected]]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, 6 months; -20°C, 1 month (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)

*"≥" 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (191.54 mM); Clear solution; Need ultrasonic

  • 2.

    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

  • 3.

    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

  • 4.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.79 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.90%

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CP-640186 hydrochloride
Cat. No.:
HY-15259A
Quantity:
MCE Japan Authorized Agent: