Haloperidol

Name: Haloperidol
Brand: MedChemExpress
SKU: HY-14538
Rating: 5.0 (14 reviews)

Cat. No.: HY-14538 Purity: 99.73%: FAQs
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Haloperidol is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic.

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

Haloperidol Chemical Structure

CAS No. : 52-86-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 106	In-stock	Estimated Time of Arrival: December 31
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5 g		Get quote

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Based on 14 publication(s) in Google Scholar

Other Forms of Haloperidol:

14 Publications Citing Use of MCE Haloperidol

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Dopamine Receptor D₁ Receptor D₂ Receptor D₃ Receptor D₄ Receptor D₅ Receptor

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Haloperidol is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic.

IC₅₀ & Target

D₂ Receptor

Cellular Effect

Cell Line	Type	Value	Description	References
5637	IC₅₀	> 20 μM Compound: Haloperidol	Cytotoxicity against human 5637 cells after 96 hrs by crystal violet staining Cytotoxicity against human 5637 cells after 96 hrs by crystal violet staining	[PMID: 19243173]
5637	IC₅₀	2.3 μM Compound: Haloperidol	Growth inhibition of human 5637 cells incubated for 96 hrs by crystal violet assay Growth inhibition of human 5637 cells incubated for 96 hrs by crystal violet assay	[PMID: 27156565]
A-427	IC₅₀	10 μM Compound: Haloperidol	Cytotoxicity against human A427 cells after 96 hrs by crystal violet staining Cytotoxicity against human A427 cells after 96 hrs by crystal violet staining	[PMID: 19243173]
A-427	IC₅₀	10 μM Compound: Haloperidol	Growth inhibition of human A427 cells after 96 hrs Growth inhibition of human A427 cells after 96 hrs	[PMID: 17967001]
A-427	IC₅₀	9.6 μM Compound: Haloperidol	Growth inhibition of human A427 cells incubated for 96 hrs by crystal violet assay Growth inhibition of human A427 cells incubated for 96 hrs by crystal violet assay	[PMID: 27156565]
CHO	IC₅₀	1.1 μM Compound: Haloperidol	Inhibition of human ERG expressed in CHO cells after 30 mins by Rb+ flux assay Inhibition of human ERG expressed in CHO cells after 30 mins by Rb+ flux assay	[PMID: 22677319]
CHO	IC₅₀	1.3 μM Compound: haloperidol	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	4.8 nM Compound: Haloperidol	Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand	[PMID: 8759642]
CHO-K1	IC₅₀	0.16 nM Compound: Haloperidol	Antagonist activity against human D2LR expressed in CHOK1 cells assessed as inhibition of pergolide-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay Antagonist activity against human D2LR expressed in CHOK1 cells assessed as inhibition of pergolide-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay	[PMID: 25126833]
DAN-G	IC₅₀	> 20 μM Compound: Haloperidol	Growth inhibition of human DAN-G cells incubated for 96 hrs by crystal violet assay Growth inhibition of human DAN-G cells incubated for 96 hrs by crystal violet assay	[PMID: 27156565]
HEK293	EC₅₀	> 10000 nM Compound: Haloperidol	Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5 Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5	[PMID: 15380206]
HEK293	IC₅₀	0.23 μM Compound: haloperidol	Inhibition of human ERG expressed in HEK293 cells coexpressing Kir2.3 after 30 mins by FluxOR based FLIPR assay Inhibition of human ERG expressed in HEK293 cells coexpressing Kir2.3 after 30 mins by FluxOR based FLIPR assay	[PMID: 22694270]
HEK293	IC₅₀	0.55 μM Compound: Haloperidol	Antagonist activity at dopamine D2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay Antagonist activity at dopamine D2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay	[PMID: 23332346]
HEK293	IC₅₀	0.7 nM Compound: Haloperidol	Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay	[PMID: 24831693]
HEK293	IC₅₀	1.16 μM Compound: Haloperidol	Inhibition of human ERG expressed in HEK293 cells measured after 30 mins by FluxOR dye based FLIPR TETRA assay Inhibition of human ERG expressed in HEK293 cells measured after 30 mins by FluxOR dye based FLIPR TETRA assay	[PMID: 32392053]
HEK293	IC₅₀	141.9 μM Compound: haloperidole	Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy	[PMID: 18788725]
HL-60	IC₅₀	> 20 μM Compound: Haloperidol	Growth inhibition of human HL60 cells incubated for 48 hrs by MTT assay Growth inhibition of human HL60 cells incubated for 48 hrs by MTT assay	[PMID: 27156565]
Jurkat	IC₅₀	0.021 μM Compound: haloperidol	Displacement of [3H]Haloperidol from sigma 1 receptor in human jurkat cells after 4 hrs Displacement of [3H]Haloperidol from sigma 1 receptor in human jurkat cells after 4 hrs	[PMID: 23403082]
Jurkat	IC₅₀	1.7 x 10^-2 μM Compound: Haloperidol	Displacement of [3H]DTG from sigma receptor in human Jurkat cells measured after 120 mins by scintillation counting method Displacement of [3H]DTG from sigma receptor in human Jurkat cells measured after 120 mins by scintillation counting method	[PMID: 27876250]
Jurkat	IC₅₀	230 nM Compound: haloperidol	Displacement of [3H](+)-pentazocine from sigma 1 opioid receptor in human Jurkat cells by scintillation counting Displacement of [3H](+)-pentazocine from sigma 1 opioid receptor in human Jurkat cells by scintillation counting	[PMID: 19875205]
LCLC-103H cell line	IC₅₀	> 20 μM Compound: Haloperidol	Cytotoxicity against human LCLC-103H cells after 96 hrs by crystal violet staining Cytotoxicity against human LCLC-103H cells after 96 hrs by crystal violet staining	[PMID: 19243173]
LCLC-103H cell line	IC₅₀	10.9 μM Compound: Haloperidol	Growth inhibition of human LCLC-103H cells incubated for 96 hrs by crystal violet assay Growth inhibition of human LCLC-103H cells incubated for 96 hrs by crystal violet assay	[PMID: 27156565]
MCF7	IC₅₀	> 20 μM Compound: Haloperidol	Growth inhibition of human MCF7 cells incubated for 96 hrs by crystal violet assay Growth inhibition of human MCF7 cells incubated for 96 hrs by crystal violet assay	[PMID: 27156565]
MCF7	IC₅₀	> 20 μM Compound: Haloperidol	Cytotoxicity against human MCF7 cells after 96 hrs by crystal violet staining Cytotoxicity against human MCF7 cells after 96 hrs by crystal violet staining	[PMID: 19243173]
MCF7	IC₅₀	20.17 μM Compound: Haloperidol	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 31042618]
MCF7	IC₅₀	24.9 μM Compound: Haloperidol	Growth inhibition of human MCF7 cells after 96 hrs Growth inhibition of human MCF7 cells after 96 hrs	[PMID: 17967001]
MCF7	IC₅₀	68 μM Compound: Halo	Cytotoxicity against ER/PR-positive HER2-negative human MCF7 cells harbouring p53 R175H mutant assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based assay Cytotoxicity against ER/PR-positive HER2-negative human MCF7 cells harbouring p53 R175H mutant assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based assay	[PMID: 35724925]
RT-4	IC₅₀	> 20 μM Compound: Haloperidol	Cytotoxicity against human RT4 cells after 96 hrs by crystal violet staining Cytotoxicity against human RT4 cells after 96 hrs by crystal violet staining	[PMID: 19243173]
RT-4	IC₅₀	16 μM Compound: Haloperidol	Growth inhibition of human RT4 cells incubated for 96 hrs by crystal violet assay Growth inhibition of human RT4 cells incubated for 96 hrs by crystal violet assay	[PMID: 27156565]
SK-BR-3	IC₅₀	131 μM Compound: Halo	Cytotoxicity against ER/PR-negative HER2-positive human SK-BR-3 cells harbouring wild type p53 assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based assay Cytotoxicity against ER/PR-negative HER2-positive human SK-BR-3 cells harbouring wild type p53 assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based assay	[PMID: 35724925]
U2OS	IC₅₀	0.06 nM Compound: Haloperidol	Antagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay Antagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay	[PMID: 25126833]

In Vivo

Haloperidol can be used to create tardive dyskinesia models. In rats, the oral half-life of Haloperidol is 5.9 hours, with a Tmax of 0.9 hours, a Cmax of 6.8 ng/mL, and an oral bioavailability of 23.0%. When administered intravenously, the AUC_0-∞ of Haloperidol is 188.4 ng·h/mL, and the t_1/2 is 2.9 hours^[3].

Induction oftardive dyskinesia^[4]

Background

Haloperidolreduces gene expression of superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GHP), thus reducing the complex cellular antioxidant defenses and increasing lipid peroxidation and nitrite/nitrate levels in the prefrontal cortex, hippocampus, and striatum^[4].

Specific Mmodeling Methods

Rat: 200-350 g • male Wistar
Administration: 1 mg/KG • i.p. • daily for 31 days

Note

Modeling Indicators

Behavior: Showed a significant reduction of locomotor activity in the open field test and also developed a cataleptic state, vacuous chewing movements (VCM), and tongue protrusion.

Correlated Product(s): /

Opposite Product(s): /

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

375.86

Formula

C₂₁H₂₃ClFNO₂

CAS No.

52-86-8

Appearance

Solid

Color

White to off-white

SMILES

ClC(C=C1)=CC=C1C2(O)CCN(CCCC(C3=CC=C(F)C=C3)=O)CC2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 40 mg/mL (106.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6606 mL	13.3028 mL	26.6057 mL
5 mM	0.5321 mL	2.6606 mL	5.3211 mL
10 mM	0.2661 mL	1.3303 mL	2.6606 mL

View the 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.67 mg/mL (4.44 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 1.67 mg/mL (4.44 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.67 mg/mL (4.44 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

mg/kg

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(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.73%

Select Batch:

Data Sheet (278 KB) SDS (584 KB)

COA (245 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Furuta Y, et al. Effects of enzyme inhibitors of catecholamine metabolism and of haloperidol on the pancreatic secretion induced by L-DOPA and by dopamine in dogs. Br J Pharmacol. 1973 Jan;47(1):77-84 [Content Brief]

[2]. Shah NS, et al. Effects of chlorpromazine and haloperidol on the disposition of mescaline-14C in mice. J Pharmacol Exp Ther. 1973 Aug;186(2):297-304 [Content Brief]

[3]. Lei K, et al. Investigation of the synergistic effects of haloperidol combined with Calculus Bovis Sativus in treating MK-801-induced schizophrenia in rats. Exp Anim. 2018 May 10;67(2):163-173. [Content Brief]

[4]. Guzen FP, et al. Haloperidol-Induced Preclinical Tardive Dyskinesia Model in Rats. Curr Protoc Neurosci. 2019 Jun;88(1):e68. [Content Brief]

Animal Administration
^[2]

Male albino mice of Swiss-Webster strain (33-36 g) are used, and all substances are given by i.p. injection in a volume of 0.5 mL. CPZ, haloperidoi and mescaline are all in time form of timeir imydrochlorides and the dose solutions are prepared at concentrations of 1.0, 0.66 and 3.3 mg/mL of 0.9% saline, respectively. The doses are: CPZ, 15 mg/kg; haloperidol, 10 mg/kg; mescaline, 50 mg/kg. Mice are pretreated with either CPZ or haloperidol 30 minutes before administration of mescaline. In some instances CPZ is injected 45 minutes after mescaline. Time animals are hmoused individually in a plexiglas cage and the gross behavior and locomotor activity. At selected intervals after mescaline, groups of mice are sacrificed by decapitation. Plasma is separated and stored at -20°C. The brain, liver, kidney, lung, spleen and heart are frozen on dry ice and stored at -20°C for 18 to 20 hours before they are used for assays.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. Furuta Y, et al. Effects of enzyme inhibitors of catecholamine metabolism and of haloperidol on the pancreatic secretion induced by L-DOPA and by dopamine in dogs. Br J Pharmacol. 1973 Jan;47(1):77-84 [Content Brief]

[2]. Shah NS, et al. Effects of chlorpromazine and haloperidol on the disposition of mescaline-14C in mice. J Pharmacol Exp Ther. 1973 Aug;186(2):297-304 [Content Brief]

[3]. Lei K, et al. Investigation of the synergistic effects of haloperidol combined with Calculus Bovis Sativus in treating MK-801-induced schizophrenia in rats. Exp Anim. 2018 May 10;67(2):163-173. [Content Brief]

[4]. Guzen FP, et al. Haloperidol-Induced Preclinical Tardive Dyskinesia Model in Rats. Curr Protoc Neurosci. 2019 Jun;88(1):e68. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6606 mL	13.3028 mL	26.6057 mL	66.5141 mL
	5 mM	0.5321 mL	2.6606 mL	5.3211 mL	13.3028 mL
	10 mM	0.2661 mL	1.3303 mL	2.6606 mL	6.6514 mL
	15 mM	0.1774 mL	0.8869 mL	1.7737 mL	4.4343 mL
	20 mM	0.1330 mL	0.6651 mL	1.3303 mL	3.3257 mL
	25 mM	0.1064 mL	0.5321 mL	1.0642 mL	2.6606 mL
	30 mM	0.0887 mL	0.4434 mL	0.8869 mL	2.2171 mL
	40 mM	0.0665 mL	0.3326 mL	0.6651 mL	1.6629 mL
	50 mM	0.0532 mL	0.2661 mL	0.5321 mL	1.3303 mL
	60 mM	0.0443 mL	0.2217 mL	0.4434 mL	1.1086 mL
	80 mM	0.0333 mL	0.1663 mL	0.3326 mL	0.8314 mL
	100 mM	0.0266 mL	0.1330 mL	0.2661 mL	0.6651 mL

Haloperidol Related Classifications

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Haloperidol52-86-8Dopamine ReceptorInhibitorinhibitorinhibit

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Haloperidol

Customer Review

Other Forms of Haloperidol:

Haloperidol Related Antibodies

14 Publications Citing Use of MCE Haloperidol

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View All Dopamine Receptor Isoform Specific Products:

Biological Activity

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References

Customer Review

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Complete Stock Solution Preparation Table

Haloperidol Related Classifications

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