1-(2-氯苯基)-N-甲基-N-(1-甲基丙基)-3-异喹啉甲酰胺

生物活性靶点体外研究

1-(2-氯苯基)-N-甲基-N-(1-甲基丙基)-3-异喹啉甲酰胺化学性质

沸点 :511.7±45.0 °C(Predicted)
密度 :1.179±0.06 g/cm3(Predicted)
储存条件 :Store at RT
溶解度 :Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 15 mg/ml).
形态 :White crystalline powder.
酸度系数(pKa) :1.76±0.50(Predicted)
颜色 :White
稳定性 :Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored under nitrogen or argon at -20° for up to 1 month.
CAS 数据库 :85532-75-8(CAS DataBase Reference)

安全信息

1-(2-氯苯基)-N-甲基-N-(1-甲基丙基)-3-异喹啉甲酰胺性质、用途与生产工艺

生物活性 PK 11195 (RP 52028) 是 TSPO 的一个配体，可靶向研究利什曼病，其对 L. amazonensis，L. major 和 L. braziliensis 的 IC50 值分别为 14.2 μM, 8.2 μM, 3.5 μM。
靶点

IC50: 14.2 μM ( L. amazonensis ), 8.2 μM ( L. major ), 3.5 μM ( L. braziliensis ) ^{[1]
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体外研究

Median IC ₅₀ values for PK 11195 are 14.2 μM for L. amazonensis , 8.2 μM for L. major , and 3.5 μM for L. braziliensis . The selective index value for L. amazonensis is 13.7, indicating the safety of PK 11195 for future testing in mammals. Time-and dose-dependent reductions in the percentage of infected macrophages, the number of parasites per infected macrophage, and the number of viable intracellular parasites are observed. Electron microscopy reveals some morphological alterations suggestive of autophagy. Interestingly, MCP-1 and superoxide levels are reduced in L. amazonensis -infected macrophages treated with PK 11195 ^{[1]
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1-(2-氯苯基)-N-甲基-N-(1-甲基丙基)-3-异喹啉甲酰胺上下游产品信息

上游原料

下游产品

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