製品番号: HY-19567

PK 11195

(別名: RP 52028)

9 Cited Publications

カスタマーレビュー

Based on 9 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.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.91%
CAS 番号: 85532-75-8
分子式: C₂₁H₂₁ClN₂O
分子量:352.86

保管条件:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

PK 11195 構造式

CAS 番号: 85532-75-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
化学情報
Publications (9)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

Leishmania

Parasite アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
C6	IC₅₀	73 μM Compound: 9, PK-11195	Cytotoxicity against rat C6 glioma cell line Cytotoxicity against rat C6 glioma cell line	[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]

体外実験

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.

化学情報

CAS 番号 85532-75-8
性状 Solid
分子量 352.86
分子式 C₂₁H₂₁ClN₂O
Color Off-white to light brown
SMILES

O=C(N(C(CC)C)C)C1=CC2=CC=CC=C2C(C3=CC=CC=C3Cl)=N1
別名

RP 52028
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (9)

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Journal Impact Factor

Pharmacol Res

SERCA2 dysfunction drives vascular calcification via coupling with TSPO-MCU at mitochondria-associated endoplasmic reticulum membranes. [Abstract]

2026 May:227:108177. PMID: 41932666
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

PK 11195 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2026 Apr:246:117733. [Abstract]

PK 11195 (20 mg/kg; IP; daily for 6 weeks) abolished the ameliorative effect of GB on retinal ferroptosis in DR mice, as evidenced by upregulated ACSL4 and downregulated Nrf2 and GPX4 protein expression in C57BL/6J mice (diabetic).

PK 11195 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2026 Apr:246:117733. [Abstract]

PK 11195 (20 mg/kg; IP; daily for 6 weeks) suppressed the expression of both TSPO and Nrf2 in the retinas of DR mice retinal sections.

PK 11195 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2026 Apr:246:117733. [Abstract]

PK 11195 (20 mg/kg; IP; daily for 6 weeks) not reversed GB attenuated the HG/PA-induced increase in albumin leakage.
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
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

PK 11195 purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2026 Feb 10:1014:178540. [Abstract]

PK 11195 (10 μM; harvested at 4 and 8 h post-LPS exposure) alone had no effect on LPS-induced IKB-α phosphorylation in HUVECs.

PK 11195 purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2026 Feb 10:1014:178540. [Abstract]

PK 11195 (5 μM; 1 h before REM administration; harvested at 4 and 8 h post-LPS exposure) fully reversed REM's suppression of this pathway in MLE-12 cells.

PK 11195 purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2026 Feb 10:1014:178540. [Abstract]

PK 11195 (10 μM; harvested at 4 and 8 h post-LPS exposure) did not alter LPS-induced mRNA expression of IL-6, IL-8, TNF-α, or IL-1β in HUVECs.

PK 11195 purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2026 Feb 10:1014:178540. [Abstract]

PK 11195 (10 μM; harvested at 4 and 8 h post-LPS exposure) had no effect on LPS-induced upregulation of ICAM-1 or VCAM-1 proteins in HUVECs.

PK 11195 purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2026 Feb 10:1014:178540. [Abstract]

PK 11195 (10 μM; 1 h before REM administration; harvested at 4 and 8 h post-LPS exposure) reversed REM-driven reductions in their expression (except ICAM-1 at 4 h post-LPS) in HUVECs.
Biochim Biophys Acta Mol Basis Dis

TSPO participates in the pathogenesis of diabetic periodontitis related to mitophagy. [Abstract]

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
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
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

溶剤 & 溶解度

体外:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8340 mL

14.1699 mL

28.3399 mL

5 mM

0.5668 mL

2.8340 mL

5.6680 mL

10 mM

0.2834 mL

1.4170 mL

2.8340 mL

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.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (276 KB)
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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

PK 11195

9 Cited Publications

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PK 11195

Anti-Infection Compound Library

Antiparasitic Compound library

Human Metabolite Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

RNA Binding Bioactive Compound Library

MedChemExpress（MCE）の使用を引用している文献 PK 11195

Parasite アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (9)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

PK 11195

Anti-Infection Compound Library

Antiparasitic Compound library

Human Metabolite Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

RNA Binding Bioactive Compound Library

MedChemExpress（MCE）の使用を引用している文献 PK 11195

Parasite アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (9)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

PK 11195 関連分類

HY-19567 関連分類