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Pizotifen

Name: Pizotifen
Brand: TargetMol
SKU: T1442
Price: 36 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T1442Cas No. 15574-96-6

Alias Pizotyline, BC-105

Pizotifen (Pizotyline) is a strong serotonin and tryptamine antagonist, with weak anticholinergic, anti-histaminic and anti-kinin effects. It also possesses sedative and appetite-stimulating properties. Pizotifen hydrochloride is an active ingredient in Sandomigran, which is used for the prophylactic management of migraine. Sandomigran is available in number of countries excluding the United States.

Pizotifen

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Purity: 99.93%

Catalog No. T1442Alias Pizotyline, BC-105Cas No. 15574-96-6

Pack Size	Price	USA Warehouse	Global Warehouse
50 mg	$36	In Stock	In Stock
100 mg	$50	In Stock	In Stock
200 mg	$71	In Stock	In Stock
500 mg	$126	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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Batch Information

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Purity:99.93%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Pizotifen AI Summary

Pizotifen exhibits a diverse range of bioactivities and pharmacological properties. It has been assessed for binding energy, showing a binding energy of 13.0 kCal mol-1 calculated using the equation deltaG obsd = -RT ln KD. This indicates its strong binding affinity to target molecules, providing insights into its potential bioactivities and interactions. In mouse models, Pizotifen demonstrates antagonism towards 5-hydroxytryptophan (5-HTP) when administered subcutaneously in doses ranging from 0.003 to 0.1 mg/kg, with an ED50 of 0.015 mg/kg after 0.5 hours. It has shown significant results in assays including modulation of Lamin A splicing, inhibition of IMPase, and potentiation by Lithium. It also inhibits malarial parasite plastid, Schwann cell viability, human tyrosyl-DNA phosphodiesterase 1, Plasmodium falciparum proliferation, and viral entry for Lassa, Marburg, and Ebola viruses. Notably, it has been identified for its gametocytocidal activity. No hepatic side effects have been detected based on the Drug-Induced Liver Injury Prediction System (DILIps), with all scores reported as 0.0 for various liver conditions, indicating minimal to no liver toxicity. Pizotifen exhibits high binding affinity towards muscarinic M1, dopamine D2, 5-HT2C, and 5-HT2B receptors (Ki values: 1.4 to 2.4 nM) and moderate affinity towards adrenergic alpha1 and 5-HT2A receptors (Ki values: 75.0 nM and 7.5 nM, respectively). It also displaces radiolabeled ligands from human 5-HT7 and 5-HT2B receptors, suggesting potent interactions with multiple neurotransmitter receptors. While it shows moderate cholestatic liver toxicity and low-frequency acute liver toxicity, it has not been predominantly associated with severe hepatic conditions like cytolytic toxicity, hepatitis, cirrhosis, or tumors. Regarding anti-parasitic and cytotoxic activities, Pizotifen has varying IC50 values across different assays, indicating potential utility against malaria, Human African Trypanosomiasis (HAT), Chagas disease, Leishmaniasis, and cytotoxicity in various cell types. For antiviral activity, it has an IC50 greater than 20,000.0 nM against SARS-CoV-2 in VERO-6 cells, implying a requirement for high concentrations for effective results. Additionally, it inhibits human HDAC6 enzyme activity, with slight inhibitory increase and a particular profile of inhibition when tested with custom versus commercial peptide substrates. Lastly, Pizotifen shows antagonist activity at human HRH1 (AC50 = 68.1 nM) and inhibits human KCNH2 (AC50 = 2307.0 nM), along with various actions at HRH2, ADRB2, HTR2A, HTR1A, ADRA1A, CNR1, and GABRA1 receptors, indicating a broad spectrum of pharmacological effects..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description

Synonyms

Pizotyline, BC-105

Chemical Properties

Molecular Weight	295.44
Formula	C₁₉H₂₁NS
Cas No.	15574-96-6
Smiles	CN1CCC(CC1)=C1c2ccsc2CCc2ccccc12
Relative Density.	1.164 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: < 0.1 mg/mL (insoluble)

DMSO: 12 mg/mL (40.62 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.77 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	3.3848 mL	16.9239 mL	33.8478 mL	169.2391 mL
5 mM	0.6770 mL	3.3848 mL	6.7696 mL	33.8478 mL
10 mM	0.3385 mL	1.6924 mL	3.3848 mL	16.9239 mL
20 mM	0.1692 mL	0.8462 mL	1.6924 mL	8.4620 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