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Ketotifen fumarate

Name: Ketotifen fumarate
Brand: TargetMol
SKU: T0994
Price: 29 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T0994Cas No. 34580-14-8

Alias HC 20511 fumarate

Ketotifen fumarate (HC 20511 fumarate) is a cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators.

Ketotifen fumarate

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Purity: 99.73%

Catalog No. T0994Alias HC 20511 fumarateCas No. 34580-14-8

Ketotifen fumarate (HC 20511 fumarate) is a cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators.

Pack Size	Price	USA Warehouse	Global Warehouse
500 mg	$40	In Stock	In Stock
1 g	$57	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$29	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:99.73%

Color:White

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COA LCMS HNMR

Product Introduction

Ketotifen fumarate AI Summary

Ketotifen fumarate demonstrates a broad spectrum of bioactivities, positioning it as a multifaceted compound with potential applications across various biological systems. It significantly inhibits degranulation in anti-DNP IgE sensitized rat RBL2H3 cells by reducing beta-hexosaminidase release after 10 minutes, exhibiting IC50 values of 220,000 nM and 158,000 nM. Additionally, it shows strong inhibitory activity at histamine H1 receptors in ddY mice, reducing histamine-induced skin vascular permeability by 98.0% at 3 mg/kg, and displays anti-inflammatory effects in BALB/c mice by inhibiting ovalbumin-induced ear swelling. Ketotifen fumarate also exhibits substantial antiplasmodial activity against Plasmodium falciparum, with IC50 values ranging from 794.33 nM to 10000.0 nM, and differential potency in various qHTS assays for inhibitors of proliferation of multiple Plasmodium falciparum lines. In terms of transport proteins, Ketotifen fumarate has high inhibitory activity in OATP1B1 and OATP1B3 transfected CHO cells. It shows antianaphylactic activity, inhibiting antigen-induced histamine release and slow-reacting substance of anaphylaxis in ovalbumin-sensitized guinea pig lung. Furthermore, it displays inhibition activity against SARS-CoV-2 by inhibiting viral-induced cytotoxicity in Vero E6 and Caco-2 cells and inhibiting 3CL-Pro protease by 17.19% at 20 µM concentration. Antifungal and antibacterial assays reveal limited inhibition against Candida albicans, Cryptococcus neoformans, and various bacterial strains, with percentages ranging from minimal to 11.46%. Additionally, it affects protein domain stability and GPCR beta-arrestin recruitment assays, displaying both inhibitory and stimulating effects on multiple receptors, signifying a complex pharmacological profile. Overall, Ketotifen fumarate is a compound of significant interest due to its wide-ranging bioactivities, implicating its potential in antiallergic, anti-inflammatory, antiplasmodial, antiviral, and possibly antifungal and antibacterial therapeutics..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Ketotifen fumarate (HC 20511 fumarate) is a cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators.
Synonyms	HC 20511 fumarate

Chemical Properties

Molecular Weight	425.50
Formula	C₂₃H₂₃NO₅S
Cas No.	34580-14-8
Smiles	OC(=O)\C=C\C(O)=O.CN1CC\C(CC1)=C1/c2ccsc2C(=O)Cc2ccccc12
Relative Density.	1.236g/cm3

Storage & Solubility Information

Storage

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

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 142.8 mg/mL (335.61 mM), Sonication is recommended.

H2O: 10.7 mg/mL (25.15 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.7 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

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3502 mL	11.7509 mL	23.5018 mL	117.5088 mL
5 mM	0.4700 mL	2.3502 mL	4.7004 mL	23.5018 mL
10 mM	0.2350 mL	1.1751 mL	2.3502 mL	11.7509 mL
20 mM	0.1175 mL	0.5875 mL	1.1751 mL	5.8754 mL

DMSO

	1mg	5mg	10mg	50mg
50 mM	0.0470 mL	0.2350 mL	0.4700 mL	2.3502 mL
100 mM	0.0235 mL	0.1175 mL	0.2350 mL	1.1751 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