Home Metabolism Acetyl-CoA carboxylase inhibitor CP 640186 For research use only.

CP 640186

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.

CP 640186 Chemical Structure

CP 640186 Chemical Structure

CAS No. 591778-68-6

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CP 640186 Related Products

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
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 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].
Animal Research Animal Models Male Sprague-Dawley rats
Dosages 5 mg/kg (IV) or 10 mg/kg (oral)
Administration IV / Oral

Chemical Information & Solubility

Molecular Weight 485.62 Formula

C30H35N3O3
CAS No. 591778-68-6 SDF --
Smiles C1CC(CN(C1)C2CCN(CC2)C(=O)C3=C4C=CC=CC4=CC5=CC=CC=C53)C(=O)N6CCOCC6
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 97 mg/mL ( (199.74 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 97 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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

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