CP 640186

For research use only.

Catalog No.S6753

CP 640186 Chemical Structure

Molecular Weight(MW): 485.62

CP 640186 is an isozyme-nonselective ACC (Acetyl-CoA carboxylase) inhibitor with IC50 values of 53 and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2, respectively.

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Choose Selective Acetyl-CoA carboxylase Inhibitors

Biological Activity

Description CP 640186 is an isozyme-nonselective ACC (Acetyl-CoA carboxylase) inhibitor with IC50 values of 53 and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2, respectively.
Targets
ACC [1]
()
55 nM
In vitro

CP-610431 inhibited ACC1 and ACC2 with IC50s of ∼50 nm. Inhibition was reversible, uncompetitive with respect to ATP, and non-competitive with respect to bicarbonate, acetyl-CoA, and citrate. CP-610431 also inhibited fatty acid synthesis, triglyceride (TG) synthesis, TG secretion, and apolipoprotein B secretion in HepG2 cells (ACC1) with EC50s of 1.6, 1.8, 3.0, and 5.7 μM, without affecting either cholesterol synthesis or apolipoprotein CIII secretion. It also inhibited both isozymes with IC50s of ∼55 nM in inhibiting HepG2 cell fatty acid and TG synthesis. CP-610431 stimulated fatty acid oxidation in C2C12 cells (ACC2) and in rat epitrochlearis muscle strips with EC50s of 57 nM and 1.3 μM[1].

In vivo

In rats, CP-640186 lowered hepatic, soleus muscle, quadriceps muscle, and cardiac muscle malonyl-CoA with ED50s of 55, 6, 15, and 8 mg/kg. Consequently, CP-640186 inhibited fatty acid synthesis in rats, CD1 mice, and ob/ob mice with ED50s of 13, 11, and 4 mg/kg, and stimulated rat whole body fatty acid oxidation with an ED50 of ∼30 mg/kg. Pharmacokinetic evaluation of CP-640186 in male Sprague-Dawley rats (intravenous dose, 5 mg/kg; oral dose, 10 mg/kg) yielded 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. At the same dose level, pharmacokinetic evaluation of CP-640186 in ob/ob mice yielded 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[1].

Protocol

Animal Research:

[1]

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  • Animal Models: Male Sprague-Dawley rats
  • Dosages: 5 mg/kg (IV) or 10 mg/kg (oral)
  • Administration: IV / Oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 97 mg/mL (199.74 mM)
Ethanol 97 mg/mL (199.74 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 485.62
Formula

C30H35N3O3

CAS No. 591778-68-6
Storage powder
in solvent
Synonyms N/A
Smiles O=C(C1CCCN(C1)C2CCN(CC2)C(=O)C3=C4C=CC=CC4=CC5=CC=CC=C35)N6CCOCC6

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Dilution Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID