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Pimozide

Name: Pimozide
Brand: TargetMol
SKU: T2546
Price: 31 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T2546Cas No. 2062-78-4

Alias R6238

Pimozide (R6238) is a diphenylbutylpiperidine derivative and a dopamine antagonist with the antipsychotic property. Pimozide selectively inhibits type 2 dopaminergic receptors in the central nervous system (CNS), thereby decreasing dopamine neurotransmission and reducing the occurrence of the motor and vocal tics and delusions of parasitosis. In addition, this agent antagonizes alpha-adrenergic and 5-HT2 receptors.

Pimozide

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Purity: 99.85%

Catalog No. T2546Alias R6238Cas No. 2062-78-4

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$31	In Stock	In Stock
50 mg	$44	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$48	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.85%

Color:White

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COA HPLC HNMR

Product Introduction

Pimozide AI Summary

Pimozide exhibits multifaceted bioactivities and binding affinities across various biological targets and systems. It shows notable binding affinity towards human 5-hydroxytryptamine receptors, specifically 5-HT6 (Ki = 71.0 nM) and rat 5-HT7 (Ki = 0.5 nM), indicating potential serotonergic effects. The compound also demonstrates high affinity towards the dopamine D2 receptor (Ki = 0.6 nM), which suggests a role in dopaminergic signaling. In terms of ion channel modulation, Pimozide is highly potent in inhibiting the human ERG potassium channel in both human embryonic kidney cells and CHO cells expressing HERG Kv11.1, with IC50 values around 18.0 nM. It also affects T-type sodium and alpha1G calcium channels, with IC50 values of 340.0 nM and 40.0 nM, respectively, highlighting its broad electrophysiological impact. Pharmacokinetically, Pimozide has a high partition coefficient (LogD = 5.42) and displays moderate oral bioavailability in humans (F = 49.0%). Furthermore, the compound exhibits significant CYP3A4 inhibition and high plasma protein binding (99.7%), which could influence its metabolic stability and distribution. Behaviorally, the compound shows efficacy in cognitive and locomotion tests in rodents, with an ED50 of 5.9 mg/kg for locomotion inhibition and impacts on passive avoidance learning. It also displays neuroleptic properties, protection against methamphetamine-induced toxicity, and reduced spontaneous motor activity. Additionally, Pimozide demonstrates potential antimicrobial activity, including antiplasmodial effects against Plasmodium falciparum and antimicrobial properties against Listeria monocytogenes. It also exhibits antiviral bioactivity, showing inhibition of SARS-CoV-2 induced cytotoxicity and protease inhibition. Overall, Pimozide presents as a versatile compound with significant activity across multiple biological pathways, including neurotransmitter receptor modulation, ion channel inhibition, antimicrobial and antiviral effects, and potential cognitive and locomotor impacts..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Pimozide (R6238) is a diphenylbutylpiperidine derivative and a dopamine antagonist with the antipsychotic property. Pimozide selectively inhibits type 2 dopaminergic receptors in the central nervous system (CNS), thereby decreasing dopamine neurotransmission and reducing the occurrence of the motor and vocal tics and delusions of parasitosis. In addition, this agent antagonizes alpha-adrenergic and 5-HT2 receptors.
Targets&IC50	D1:588 nM (Ki), D2:1.4 nM (Ki), α1-adrenoceptor:39 nM (Ki), D3:2.5 nM (Ki)
Synonyms	R6238

Chemical Properties

Molecular Weight	461.55
Formula	C₂₈H₂₉F₂N₃O
Cas No.	2062-78-4
Smiles	Fc1ccc(cc1)C(CCCN1CCC(CC1)n1c2ccccc2[nH]c1=O)c1ccc(F)cc1
Relative Density.	1.1763 g/cm3 (Estimated)

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 41 mg/mL (88.83 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.17 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1666 mL	10.8331 mL	21.6661 mL	108.3306 mL
5 mM	0.4333 mL	2.1666 mL	4.3332 mL	21.6661 mL
10 mM	0.2167 mL	1.0833 mL	2.1666 mL	10.8331 mL
20 mM	0.1083 mL	0.5417 mL	1.0833 mL	5.4165 mL
50 mM	0.0433 mL	0.2167 mL	0.4333 mL	2.1666 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc