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CP640186
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。
CP640186图片
CAS NO:591778-68-6
规格:≥98%
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
CP-640186 is a novel, potent and and cell-permeable inhibitor of mammalian ACCs (isozyme-nonselective acetyl-CoA carboxylase) with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively; It hash improved metabolic stability in comparison to CP-610431, an analog of CP-640186. Inhibition of ACC, with its resultant inhibition of fatty acid synthesis and stimulation of fatty acid oxidation, has the potential to favorably affect the multitude of cardiovascular risk factors associated with the metabolic syndrome. CP-640186 can reduce body weight and improve insulin sensitivity in test animals. CP-640186, also inhibited both isozymes with IC50s of ~55 nM but was 2–3 times more potent than CP-610431 in inhibiting HepG2 cell fatty acid and TG synthesis. CP-640186 also stimulated fatty acid oxidation in C2C12 cells (ACC2) and in rat epitrochlearis muscle strips with EC50s of 57 nM and 1.3 uM.
理化性质和储存条件
Molecular Weight (MW)485.62
FormulaC30H35N3O3
CAS No.591778-68-6 (free base)
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 10 mM
Water: <1 mg/mL
Ethanol: N/A
SMILES CodeO=C(C1=C2C=CC=CC2=CC3=CC=CC=C13)N4CCC(N5C[C@H](C(N6CCOCC6)=O)CCC5)CC4
SynonymsCP 640186; CP640,186; CP640186; CP-640186; CP-640,186; CP 640,186.
实验参考方法
In Vitro

In vitro activity: CP-640186 HCl is a potent inhibitor of mammalian ACCs (isozyme-nonselective acetyl-CoA carboxylase) with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively; It hash improved metabolic stability in comparison to CP-610431, an analog of CP-640186. CP-640186 can reduce body weight and improve insulin sensitivity in test animals. CP-640186, also inhibited both isozymes with IC50s of ~55 nM but was 2–3 times more potent than CP-610431 in inhibiting HepG2 cell fatty acid and TG synthesis. CP-640186 also stimulated fatty acid oxidation in C2C12 cells (ACC2) and in rat epitrochlearis muscle strips with EC50s of 57 nM and 1.3 uM. C

Kinase Assay: CP-640186 HCl is a potent inhibitor of mammalian ACCs (isozyme-nonselective acetyl-CoA carboxylase) with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively.

Cell Assay: P-640186, also inhibited both isozymes with IC50s of ~55 nM but was 2–3 times more potent than CP-610431 in inhibiting HepG2 cell fatty acid and TG synthesis. CP-640186 also stimulated fatty acid oxidation in C2C12 cells (ACC2) and in rat epitrochlearis muscle strips with EC50s of 57 nM and 1.3 uM

In VivoIn 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
Animal modelRats and mice
Formulation & Dosage6, 15, and 8 mg/kg (Rat); 13, 11, and 4 mg/kg (mice)
References J Biol Chem. 2003 Sep 26;278(39):37099-111. Epub 2003 Jul 3.