Cat. No.: HY-12987

Pimozide

(Synonyms: R6238)

6 Cited Publications

Customer Review

Based on 6 publication(s) in Google Scholar

Pimozide is a dopamine receptor antagonist, with K_is 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 K_i of 39 nM; Pimozide also inhibits STAT3 and STAT5.

For research use only. We do not sell to patients.

Purity: 99.94%
CAS No.: 2062-78-4
Formula: C₂₈H₂₉F₂N₃O
Molecular Weight:461.55

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Pimozide Chemical Structure

CAS No.: 2062-78-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Publications (6)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]^[2]^[3]

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

All Dopamine Receptor Isoforms :

All Adrenergic Receptor Isoforms :

All STAT Isoforms :

All Parasite Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.24 μM Compound: pimozide	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	[PMID: 23812503]
CHO	IC₅₀	0.34 μM Compound: Pimozide	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	[PMID: 8691482]
CHO	IC₅₀	18 nM Compound: pimozide	Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1 Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1	[PMID: 12729675]
HCT-116	IC₅₀	10 μM Compound: 95	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	[PMID: 33445154]
HEK293	IC₅₀	>500 μM Compound: pimozide	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	[PMID: 23241029]
HEK293	IC₅₀	>500 μM Compound: pimozide	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	[PMID: 23241029]
HEK293	IC₅₀	34.2 μM Compound: pimozide	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	[PMID: 23241029]
K562	IC₅₀	5 μM Compound: 1	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	[PMID: 25131537]
LLC-PK1	IC₅₀	>50 μM Compound: Pimozide	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	[PMID: 12699389]
LLC-PK1	IC₅₀	>50 μM Compound: Pimozide	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	[PMID: 12699389]
LLC-PK1	IC₅₀	2.9 μM Compound: Pimozide	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	[PMID: 12699389]
LLC-PK1	IC₅₀	2.9 μM Compound: Pimozide	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	[PMID: 12699389]
LLC-PK1	IC₅₀	4.9 μM Compound: Pimozide	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	[PMID: 12699389]
LLC-PK1	IC₅₀	4.9 μM Compound: Pimozide	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	[PMID: 12699389]
SW480	IC₅₀	10 μM Compound: 95	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	[PMID: 33445154]

In Vitro

Pimozide is a dopamine receptor antagonist, with K_is 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 K_is 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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 2062-78-4
Appearance Solid
Molecular Weight 461.55
Formula C₂₈H₂₉F₂N₃O
Color White to off-white
SMILES

O=C1NC2=CC=CC=C2N1C3CCN(CCCC(C4=CC=C(F)C=C4)C5=CC=C(F)C=C5)CC3
Synonyms

R6238
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (6)

All Bio/Physico-chemical AssayCell Imaging/StainingCell Migration/Invasion AssayIn Vivo Efficacy StudyWB

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Journal Impact Factor

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
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.
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.
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
Biochem Biophys Res Commun

Dual-cardiotoxicity evaluation of torsadogenic risk drugs using human iPSC-derived cardiomyocytes. [Abstract]

2025 Oct 30:786:152756. PMID: 41043280
bioRxiv

2024 November 28.

Solvent & Solubility

In Vitro:

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)

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

2.1666 mL

10.8331 mL

21.6661 mL

5 mM

0.4333 mL

2.1666 mL

4.3332 mL

10 mM

0.2167 mL

1.0833 mL

2.1666 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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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Volume _(start) Volume _(start)

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In Vivo:

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: ≥ 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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.67 mg/mL (3.62 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL Corn oil, 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

Protocol

Cell Assay^[2]

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.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
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)
- Korean - KR (397 KB)
- Portuguese - PT (397 KB)
COA (2659 KB)
Elemental Analysis Report (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)
Handling Instructions (2659 KB)

References

[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]

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	2.1666 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

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Pimozide

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Publications Citing Use of MedChemExpress (MCE) Pimozide

All Dopamine Receptor Isoforms

All Adrenergic Receptor Isoforms

All STAT Isoforms

All Parasite Isoforms

Biological Activity

Chemical Information

Publications (6)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Pimozide Related Classifications

Cat. No.: HY-12987