PK 11195
Based on 8 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.91%
- CAS No.: 85532-75-8
- Formula: C21H21ClN2O
- Molecular Weight:352.86
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) PK 11195
More- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- Biochem Pharmacol. 2026 Apr:246:117733. [Abstract]
- Eur J Pharmacol. 2026 Feb 10:1014:178540. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2025 Apr 23;1871(6):167866. [Abstract]
- Exp Neurol. 2023 Nov:369:114542. [Abstract]
- J Inflamm. 2024 Apr 19;21(1):11. [Abstract]
- Exp Cell Res. 2025 Jul 15;450(2):114674. [Abstract]
- Metab Brain Dis. 2025 Mar 6;40(3):137. [Abstract]
All Parasite Isoforms
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Biological Activity
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Leishmania |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| C6 | IC50 |
73 μM
Compound: 9, PK-11195
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Cytotoxicity against rat C6 glioma cell line
Cytotoxicity against rat C6 glioma cell line
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[PMID: 16970409] |
| HEK-293T | IC50 |
>100 μM
Compound: PK 11195
|
Antiproliferative activity against HEK293T cells expressing human TSPO A147T mutant after 48 hrs by BrdU incorporation assay
Antiproliferative activity against HEK293T cells expressing human TSPO A147T mutant after 48 hrs by BrdU incorporation assay
|
[PMID: 30108706] |
| HEK-293T | IC50 |
>100 μM
Compound: PK 11195
|
Antiproliferative activity against HEK293T cells expressing human wild type TSPO after 48 hrs by BrdU incorporation assay
Antiproliferative activity against HEK293T cells expressing human wild type TSPO after 48 hrs by BrdU incorporation assay
|
[PMID: 30108706] |
| HEK-293T | IC50 |
67.4 μM
Compound: PK 11195
|
Cytotoxicity against HEK293T cells expressing human wild type TSPO assessed as decrease in cell viability after 48 hrs by CellTiter blue assay
Cytotoxicity against HEK293T cells expressing human wild type TSPO assessed as decrease in cell viability after 48 hrs by CellTiter blue assay
|
[PMID: 30108706] |
| HEK-293T | IC50 |
69.15 μM
Compound: PK 11195
|
Cytotoxicity against HEK293T cells expressing human TSPO A147T mutant assessed as decrease in cell viability after 48 hrs by CellTiter blue assay
Cytotoxicity against HEK293T cells expressing human TSPO A147T mutant assessed as decrease in cell viability after 48 hrs by CellTiter blue assay
|
[PMID: 30108706] |
| Jurkat | EC50 |
56 μM
Compound: PK, PK-11195
|
Induction of reactive oxygen species response in Jurkat cells after 1 hr
Induction of reactive oxygen species response in Jurkat cells after 1 hr
|
[PMID: 17251020] |
| Jurkat | EC50 |
75 μM
Compound: PK, PK-11195
|
Induction of cell death in Jurkat cells after 24 hrs
Induction of cell death in Jurkat cells after 24 hrs
|
[PMID: 17251020] |
| MCF7 | IC50 |
5.4 nM
Compound: PK11195
|
Antiproliferative activity against human MCF7 assessed as inhibition of cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human MCF7 assessed as inhibition of cell viability incubated for 72 hrs by CCK-8 assay
|
[PMID: 32942072] |
| Ramos | EC50 |
>80 μM
Compound: PK-11195
|
Lymphotoxic activity against immortalized Ramos B cells in culture
Lymphotoxic activity against immortalized Ramos B cells in culture
|
[PMID: 12951119] |
| Ramos | EC50 |
100 μM
Compound: PK, PK-11195
|
Induction of reactive oxygen species response in Ramos cells after 1 hr
Induction of reactive oxygen species response in Ramos cells after 1 hr
|
[PMID: 17251020] |
| Ramos | EC50 |
90 μM
Compound: PK, PK-11195
|
Induction of cell death in Ramos cells after 24 hrs
Induction of cell death in Ramos cells after 24 hrs
|
[PMID: 17251020] |
| T47D | IC50 |
6 nM
Compound: PK11195
|
Antiproliferative activity against human T47D assessed as inhibition of cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human T47D assessed as inhibition of cell viability incubated for 72 hrs by CCK-8 assay
|
[PMID: 32942072] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 85532-75-8
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Appearance Solid
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Molecular Weight 352.86
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Formula C21H21ClN2O
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Color Off-white to light brown
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SMILES
O=C(N(C(CC)C)C)C1=CC2=CC=CC=C2C(C3=CC=CC=C3Cl)=N1
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Synonyms
RP 52028
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (8)
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Journal Impact Factor
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Most Recent
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Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Biochem Pharmacol
Ginkgolide B alleviates diabetic retinopathy by inhibiting ferroptosis in retinal vascular endothelial cells via the TSPO/Nrf2 pathway. [Abstract]2026 Apr:246:117733. PMID: 41571203 -
Eur J Pharmacol
Remimazolam alleviates acute lung injury via translocator protein mediated inhibition of the NF-κB pathway. [Abstract]2026 Feb 10:1014:178540. PMID: 41519458 -
Biochim Biophys Acta Mol Basis Dis
2025 Apr 23;1871(6):167866. PMID: 40280203 -
Exp Neurol
TSPO exacerbates acute cerebral ischemia/reperfusion injury by inducing autophagy dysfunction. [Abstract]2023 Nov:369:114542. PMID: 37717810 -
J Inflamm
Mitochondria protective and anti-apoptotic effects of peripheral benzodiazepine receptor and its ligands on the treatment of asthma in vitro and vivo. [Abstract]2024 Apr 19;21(1):11. PMID: 38641850 -
Exp Cell Res
The effect of TSPO transmembrane transport-mediated paeonol mitochondrial antioxidant on dexamethasone-induced mitochondrial abnormalities, oxidative stress damage, and apoptosis in SV40-MES-13 cells. [Abstract]2025 Jul 15;450(2):114674. PMID: 40683587 -
Metab Brain Dis
The impact and mechanisms of YL-IPA08, a potent ligand for the translocator protein (18 kDa) on protection against LPS-induced depression and cognitive dysfunction in rodents. [Abstract]2025 Mar 6;40(3):137. PMID: 40047959
Solvent & Solubility
DMSO : 25 mg/mL (70.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.89 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.89 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8340 mL | 14.1699 mL | 28.3399 mL | 70.8496 mL |
| 5 mM | 0.5668 mL | 2.8340 mL | 5.6680 mL | 14.1699 mL | |
| 10 mM | 0.2834 mL | 1.4170 mL | 2.8340 mL | 7.0850 mL | |
| 15 mM | 0.1889 mL | 0.9447 mL | 1.8893 mL | 4.7233 mL | |
| 20 mM | 0.1417 mL | 0.7085 mL | 1.4170 mL | 3.5425 mL | |
| 25 mM | 0.1134 mL | 0.5668 mL | 1.1336 mL | 2.8340 mL | |
| 30 mM | 0.0945 mL | 0.4723 mL | 0.9447 mL | 2.3617 mL | |
| 40 mM | 0.0708 mL | 0.3542 mL | 0.7085 mL | 1.7712 mL | |
| 50 mM | 0.0567 mL | 0.2834 mL | 0.5668 mL | 1.4170 mL | |
| 60 mM | 0.0472 mL | 0.2362 mL | 0.4723 mL | 1.1808 mL |