PZ0362
CP-640186 盐酸盐
≥95% (HPLC)
别名:
CP 640186 盐酸盐, CP640186 盐酸盐, [(3R)-1′-(9-蒽基羰基)[1,4′-联哌啶] -3-基] -4-吗啉基-甲酮 盐酸盐, （3R）-蒽-9-基-[3-（吗啉-4-羰基）-[1,4 ′]双哌啶基-1′-基]-甲酮 盐酸盐
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关于此项目
经验公式（希尔记法）:
C30H35N3O3 · HCl
化学文摘社编号:
分子量:
522.08
UNSPSC Code:
41121800
NACRES:
NA.77
MDL number:
InChI
1S/C30H35N3O3.ClH/c34-29(32-16-18-36-19-17-32)24-8-5-13-33(21-24)25-11-14-31(15-12-25)30(35)28-26-9-3-1-6-22(26)20-23-7-2-4-10-27(23)28;/h1-4,6-7,9-10,20,24-25H,5,8,11-19,21H2;1H/t24-;/m1./s1
SMILES string
O=C(C1=C2C=CC=CC2=CC3=CC=CC=C31)N(CC4)CCC4N5C[C@H](C(N6CCOCC6)=O)CCC5.[H]Cl
InChI key
DUBNXJIOBFRASV-GJFSDDNBSA-N
assay
≥95% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
H2O: 2 mg/mL, clear (warmed)
storage temp.
room temp
Quality Level
Application
CP-640186盐酸盐已用作变构乙酰辅酶A羧化酶（ACC）抑制剂（ACCi），以药理抑制脂肪生成，进而确定脂肪酸合成是否对棕色脂肪组织（BAT）变白至关重要。它还可用作哺乳动物乙酰辅酶A羧化酶（mACC1/2）的抑制剂，以研究其对美洛培南药效抗多种病原体的作用，包括泰国伯克霍尔德菌、铜绿假单胞菌、鼠伤寒沙门氏菌和减毒鼠疫杆菌等。
Biochem/physiol Actions
CP-640186是一种有效的具有口服活性的乙酰辅酶A羧化酶1/2（ACC-alpha/beta，ACC1/2）抑制剂（IC50〜50 nM），其可靶向ACC二聚体界面处的羧基转移酶（CT）结构域（通过紧密与假定的生物素结合位点之间的相互作用），且具有可逆性，对于ATP、碳酸氢盐、乙酰辅酶A和柠檬酸不具有竞争性。CP-610431可抑制脂肪酸（FA）的合成、甘油三酸酯（TG）的合成、TG和apoB的分泌（IC50分别为1.6、1.8、3.0和5.7 μM），但不影响HepG2细胞（ACC1）中胆固醇的合成或apoC3的分泌，同时其还可以刺激C2C12细胞（ACC2）和大鼠棘上肌条中FA的氧化（EC50分贝为57 nM和1.3 μM）。口服可抑制大鼠、CD1小鼠和ob/ob小鼠的FA合成（ED50分别为13、11和4 mg/kg），同时在体内还可刺激大鼠全身FA氧化（ED50为∼30 mg/kg）。
存储类别
11 - Combustible Solids
wgk
WGK 3
Yasunori Nio et al.
Antiviral research, 132, 262-267 (2016-07-10)
Recently, direct antiviral agents against hepatitis C virus (HCV) infection have been developed as highly effective anti-HCV drugs. However, the appearance of resistant viruses against direct anti-viral agents is an unsolved problem. One of the strategies considered to suppress the
P B Patil et al.
Archives of physiology and biochemistry, 113(1), 13-24 (2007-05-25)
There seems to be an association between increased concentrations of malonyl coenzyme A (malonyl CoA) in skeletal muscle and diabetes and/or insulin resistance. The purpose of the current study was to test the hypothesis that treatments designed to manipulate malonyl
Hailong Zhang et al.
Structure (London, England : 1993), 12(9), 1683-1691 (2004-09-03)
Acetyl-coenzyme A carboxylases (ACCs) are important targets for the development of therapeutic agents against obesity, diabetes, and other diseases. CP-640186 is a potent inhibitor of mammalian ACCs and can reduce body weight and improve insulin sensitivity in test animals. It
Deepa S Valsangkar et al.
Molecular reproduction and development, 82(9), 679-693 (2015-06-05)
In mouse oocytes, meiotic induction by pharmacological activation of PRKA (adenosine monophosphate-activated protein kinase; formerly known as AMPK) or by hormones depends on stimulation of fatty acid oxidation (FAO). PRKA stimulates FAO by phosphorylating and inactivating acetyl CoA carboxylase (ACAC;
Kevin P Madauss et al.
Acta crystallographica. Section D, Biological crystallography, 65(Pt 5), 449-461 (2009-04-25)
Inhibition of acetyl-CoA carboxylase (ACC) may prevent lipid-induced insulin resistance and type 2 diabetes, making the enzyme an attractive pharmaceutical target. Although the enzyme is highly conserved amongst animals, only the yeast enzyme structure is available for rational drug design.
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