PK 11195

A high affinity ligand for peripheral benzodiazepine receptor, TSPO

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库存: 现货

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5mg

￥600.00

480.00

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10mg

￥812.00

650.00

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50mg

￥2725.00

2180.00

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100mg

￥4850.00

3880.00

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货号: ajci17380
CAS: 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
分子式: C21H21ClN2O
分子量: 352.86
纯度: >98%
溶解度: Acetonitrile: 10 mg/ml,Chloroform: 33 mg/ml,Methanol: 16 mg/ml
储存: Store at -20°C
库存: 现货

Background

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].

参考文献:
[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.