ピモジド
Based on 8 publication(s) in Google Scholar
Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
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- 純度: 99.94%
- CAS 番号: 2062-78-4
- 分子式: C28H29F2N3O
- 分子量:461.55
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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MedChemExpress（MCE）の使用を引用している文献 Pimozide
More- Nat Chem Biol. 2026 May 27. [Abstract]
- Cell Chem Biol. 2021 Jun 17;28(6):855-865.e9. [Abstract]
- Int Immunopharmacol. 2020 Jul:84:106500. [Abstract]
- Biochem Biophys Res Commun. 2025 Oct 30:786:152756. [Abstract]
- Elife. 2026 Jun 22:15:RP109081. [Abstract]
- Elife. 2025 Aug 28:14:RP104774. [Abstract]
- bioRxiv. 2024 November 28.
- Bioengineered. 2022 Apr;13(4):11083-11095. [Abstract]
Customer Validation & Images
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WB
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Bio/Physico-chemical Assay
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Cell Imaging/Staining
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Cell Migration/Invasion Assay
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In Vivo Efficacy Study
Dopamine Receptor アイソフォーム固有の製品をすべて表示
MoreAdrenergic Receptor アイソフォーム固有の製品をすべて表示
MoreParasite アイソフォーム固有の製品をすべて表示
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生物活性
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Dopamine D2 receptor 1.4 nM (Ki) |
Dopamine D3 receptor 2.5 nM (Ki) |
Dopamine D1 receptor 588 nM (Ki) |
α1-adrenoceptor 39 nM (Ki) |
STAT3 |
STAT5 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.24 μM
Compound: pimozide
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Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
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[PMID: 23812503] |
| CHO | IC50 |
0.34 μM
Compound: Pimozide
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Inhibitory activity against type IIA sodium channel in CNaIIA-1 cell line expressed in CHO cells
Inhibitory activity against type IIA sodium channel in CNaIIA-1 cell line expressed in CHO cells
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[PMID: 8691482] |
| CHO | IC50 |
18 nM
Compound: pimozide
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Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1
Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1
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[PMID: 12729675] |
| HCT-116 | IC50 |
10 μM
Compound: 95
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Antiproliferative activity against human HCT-116 cells assessed as reduction in cell proliferation incubated for 12 to 24 hrs by CCK-8 assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell proliferation incubated for 12 to 24 hrs by CCK-8 assay
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[PMID: 33445154] |
| HEK293 | IC50 |
>500 μM
Compound: pimozide
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Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
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[PMID: 23241029] |
| HEK293 | IC50 |
>500 μM
Compound: pimozide
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Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
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[PMID: 23241029] |
| HEK293 | IC50 |
34.2 μM
Compound: pimozide
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Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
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[PMID: 23241029] |
| K562 | IC50 |
5 μM
Compound: 1
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Cytotoxicity against human K562 cells after 48 hrs by trypan blue dye exclusion test
Cytotoxicity against human K562 cells after 48 hrs by trypan blue dye exclusion test
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[PMID: 25131537] |
| LLC-PK1 | IC50 |
>50 μM
Compound: Pimozide
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Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
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[PMID: 12699389] |
| LLC-PK1 | IC50 |
>50 μM
Compound: Pimozide
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TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells
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[PMID: 12699389] |
| LLC-PK1 | IC50 |
2.9 μM
Compound: Pimozide
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Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
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[PMID: 12699389] |
| LLC-PK1 | IC50 |
2.9 μM
Compound: Pimozide
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TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells
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[PMID: 12699389] |
| LLC-PK1 | IC50 |
4.9 μM
Compound: Pimozide
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Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
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[PMID: 12699389] |
| LLC-PK1 | IC50 |
4.9 μM
Compound: Pimozide
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TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells
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[PMID: 12699389] |
| SW480 | IC50 |
10 μM
Compound: 95
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Antiproliferative activity against human SW480 cells assessed as reduction in cell proliferation incubated for 12 to 24 hrs by CCK-8 assay
Antiproliferative activity against human SW480 cells assessed as reduction in cell proliferation incubated for 12 to 24 hrs by CCK-8 assay
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[PMID: 33445154] |
Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively; also has affinity at α1-adrenoceptor and 5-HT1A, with Kis of 39 nM and 310 nM, respectively[1]. Pimozide acts as an inhibitor of STAT3. Pimozide (0-15 μM) shows inhibitory of the proliferation of U2OS cells, with IC50 value at 24, 48, and 72 h of 22.16 ± 2.54, 17.49 ± 1.14 and 13.78 ± 0.34 μM, respectively. Pimozide (10 μM) inhibits the colony- and sphere-forming abilities of osteosarcoma cells. Pimozide (15 μM) induces G0/G1 phase cell cycle arrest, suppresses the extracellular signal-regulated kinase (Erk) signaling to inhibit cell viability, and produces ROS generation through inhibiting antioxidant enzyme gene catalase expression in osteosarcoma cells[2]. Pimozide acts as an inhibitor of STAT5. Pimozide reduces the expression of endogenous STAT5 target genes, and decreases STAT5 tyrosine phosphorylation[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2062-78-4
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性状 Solid
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分子量 461.55
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分子式 C28H29F2N3O
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Color White to off-white
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SMILES
O=C1NC2=CC=CC=C2N1C3CCN(CCCC(C4=CC=C(F)C=C4)C5=CC=C(F)C=C5)CC3
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別名
Pimozide; R6238
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 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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Nat Chem Biol
2026 May 27. PMID: 42204309 -
Cell Chem Biol
Development of potent and selective inhibitors targeting the papain-like protease of SARS-CoV-2. [Abstract]2021 Jun 17;28(6):855-865.e9. PMID: 33979649 -
Int Immunopharmacol
The antipsychotic drug pimozide inhibits IgE-mediated mast cell degranulation and migration. [Abstract]2020 Jul:84:106500. PMID: 32311669
Pimozide purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2020 Jul:84:106500. [Abstract]
Pimozide (10-40 μM; 1 h) treatment reduced the released levels of the granule-related mediator β-hexosaminidase dose-dependently in DNP-HSA-activated RBLs and BMMCs.
Pimozide purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2020 Jul:84:106500. [Abstract]
Pimozide (10-20 μM; 1 h) significantly inhibited the morphological changes and purple granule release of IgE/Ag-activated RBLs.
Pimozide purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2020 Jul:84:106500. [Abstract]
Pimozide (10-20 μM; 1 h) pretreatment reduced the migration-augmenting effect of IgE/Ag induction on RBLs in a dose-dependent manner.
Pimozide purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2020 Jul:84:106500. [Abstract]
Pimozide (10–20 mg/kg; 1 h; i.p.) treatment decreased the PCA reaction of mice markedly induced by IgE/Ag, as evidenced by a reduced ear thickness and diminished extrusion of dye from injected ears compared to the activated group.
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Biochem Biophys Res Commun
Dual-cardiotoxicity evaluation of torsadogenic risk drugs using human iPSC-derived cardiomyocytes. [Abstract]2025 Oct 30:786:152756. PMID: 41043280 -
Elife
Dopamine and its receptor DcDop2 are involved in the coevolution between ' Candidatus Liberibacter asiaticus' and Diaphorina citri. [Abstract]2026 Jun 22:15:RP109081. PMID: 42329805 -
Elife
Enalapril mitigates senescence and aging-related phenotypes in human cells and mice via pSmad1/5/9-driven antioxidative genes. [Abstract]2025 Aug 28:14:RP104774. PMID: 40874922
Pimozide purchased from MedChemExpress. Usage Cited in: Elife. 2025 Aug 28:14:RP104774. [Abstract]
ID1 inhibitor Pimozide (5 μM; 3 d) resulted in a decreasing trend of ID1 expression and a significant increase in p16 and p21 expression in IMR90 cells.
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Bioengineered
The long non-coding RNA T cell leukemia homeobox 1 neighbor enhances signal transducer and activator of transcription 5A phosphorylation to promote colon cancer cell invasion, migration, and metastasis. [Abstract]2022 Apr;13(4):11083-11095. PMID: 35502613
溶剤 & 溶解度
DMSO : 16.67 mg/mL (36.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 1.67 mg/mL (3.62 mM); Clear solution
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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: 1.67 mg/mL (3.62 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
プロトコル
Cell proliferation is assessed by WST-8 colorimetric assay. Human osteosarcoma cells are plated in 96-well plates with 2,500 cells per well and exposed to the treatment of different concentrations of pimozide for various time intervals (24 h, 48 h, and 72 h). The WST-8 solution is added to each well after indicated time. After incubated at 37°C for another 4 hours, the absorbance ismeasured at 450 nm using a multi-well plate reader[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (279 KB)
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SDS (397 KB)
- English - EN (397 KB)
- Français - FR (397 KB)
- Deutsch - DE (397 KB)
- Norwegian - NO (397 KB)
- Español - ES (397 KB)
- Swedish - SV (397 KB)
- Italian - IT (397 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Ybema CE, et al. Adrenoceptors and dopamine receptors are not involved in the discriminative stimulus effect of the 5-HT1A receptor agonist flesinoxan. Eur J Pharmacol. 1994 Apr 21;256(2):141-7. [Content Brief]
[2]. Cai N, et al. The STAT3 inhibitor pimozide impedes cell proliferation and induces ROS generation in human osteosarcoma by suppressing catalase expression. Am J Transl Res. 2017 Aug 15;9(8):3853-3866. eCollection 2017. [Content Brief]
[3]. Erik A. Nelson, et al. The STAT5 inhibitor pimozide decreases survival of chronic myelogenous leukemia cells resistant to kinase inhibitors. Blood. 2011 Mar 24; 117(12): 3421-3429. [Content Brief]
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 | 2.1666 mL | 10.8331 mL | 21.6661 mL | 54.1653 mL |
| 5 mM | 0.4333 mL | 2.1666 mL | 4.3332 mL | 10.8331 mL | |
| 10 mM | 0.2167 mL | 1.0833 mL | 2.1666 mL | 5.4165 mL | |
| 15 mM | 0.1444 mL | 0.7222 mL | 1.4444 mL | 3.6110 mL | |
| 20 mM | 0.1083 mL | 0.5417 mL | 1.0833 mL | 2.7083 mL | |
| 25 mM | 0.0867 mL | 0.4333 mL | 0.8666 mL | 2.1666 mL | |
| 30 mM | 0.0722 mL | 0.3611 mL | 0.7222 mL | 1.8055 mL |
Pimozide 関連分類
HY-12987 関連分類
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