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PK 11195
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。
PK 11195图片
CAS NO:85532-75-8
包装与价格：
包装价格(元)
50mg询价
10mg询价

PK 11195 (RP 52028) 是转运蛋白 (TSPO) 的配体，靶向利什曼原虫化疗，对利什曼原虫的 IC50 分别为 14.2 μM、8.2 μM、3.5 μM。
Cas No.85532-75-8
别名1-(2-氯苯基)-N-甲基-N-(1-甲基丙基)-3-异喹啉甲酰胺,RP 52028
化学名(R)-N-(sec-butyl)-1-(2-chlorophenyl)-N-methylisoquinoline-3-carboxamide
Canonical SMILESClC1=CC=CC=C1C2=C(C=CC=C3)C3=CC(C(N(C)[C@H](C)CC)=O)=N2
分子式C21H21ClN2O
分子量352.86
溶解度Acetonitrile: 10 mg/ml,Chloroform: 33 mg/ml,Methanol: 16 mg/ml
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

PK 11195 (RP 52028) is a ligand of translocator protein (TSPO), which targets Leishmania chemotherapy, with IC50s of 14.2 μM, 8.2 μM, 3.5 μM for L. amazonensis, L. major and L. braziliensis, respectively.

Median IC50 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].

References:
[1]. Guedes CES, et al. In vitro evaluation of the anti-leishmanial activity and toxicity of PK-11195. Mem Inst Oswaldo Cruz. 2018 Feb 5;113(4):e170345.

 
 
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