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
H James Harwood et al.
The Journal of biological chemistry, 278(39), 37099-37111 (2003-07-05)
Inhibition of acetyl-CoA carboxylase (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. To achieve maximal effectiveness
Hitomi Okamura et al.
Biochemical and biophysical research communications, 475(1), 87-92 (2016-05-15)
Hepatitis B virus (HBV) proliferates in hepatocytes after infection, but the host factors that contribute to the HBV lifecycle are poorly understood at the molecular level. We investigated whether fatty acid biosynthesis (FABS), which was recently reported to contribute to
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
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.
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
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