PK 11195 (Synonyms: RP 52028) |
| Catalog No.GC16569 |
PK 11195 (RP 52028) es un ligando de la proteÍna translocadora (TSPO), que se dirige a la quimioterapia de Leishmania, con IC50 de 14,2 μM, 8,2 μM, 3,5 μM para L.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 85532-75-8
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 85532-75-8 | SDF | |
| Sinónimos | RP 52028 | ||
| Chemical Name | (R)-N-(sec-butyl)-1-(2-chlorophenyl)-N-methylisoquinoline-3-carboxamide | ||
| Canonical SMILES | ClC1=CC=CC=C1C2=C(C=CC=C3)C3=CC(C(N(C)[C@H](C)CC)=O)=N2 | ||
| Formula | C21H21ClN2O | M.Wt | 352.86 |
| Solubility | Acetonitrile: 10 mg/ml,Chloroform: 33 mg/ml,Methanol: 16 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.834 mL | 14.1699 mL | 28.3399 mL |
| 5 mM | 0.5668 mL | 2.834 mL | 5.668 mL |
| 10 mM | 0.2834 mL | 1.417 mL | 2.834 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)
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