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品質等級
化驗
≥95% (HPLC)
形狀
powder
儲存條件
desiccated
顏色
white to beige
溶解度
H2O: 2 mg/mL, clear (warmed)
儲存溫度
room temp
SMILES 字串
O=C(C1=C2C=CC=CC2=CC3=CC=CC=C31)N(CC4)CCC4N5C[C@H](C(N6CCOCC6)=O)CCC5.[H]Cl
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
InChI 密鑰
DUBNXJIOBFRASV-GJFSDDNBSA-N
應用
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。
生化／生理作用
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）。
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
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