Cat. No.: HY-B0157A

Ketotifen fumarate

(Synonyms: HC 20511 fumarate)

3 Cited Publications

Customer Review

Based on 3 publication(s) in Google Scholar

Ketotifen (HC 20-511) fumarate is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen fumarate can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen fumarate also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen fumarate can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention.

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

Purity: 99.88%
CAS No.: 34580-14-8
Formula: C₂₃H₂₃NO₅S
Molecular Weight:425.50

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Ketotifen fumarate Chemical Structure

CAS No.: 34580-14-8

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

H₁ Receptor

All Histamine Receptor Isoforms :

All Endogenous Metabolite Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	1 nM Compound: Ketotifen	Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting	[PMID: 21470866]
CHO-K1	IC₅₀	1 nM Compound: 38	Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting	[PMID: 19362477]
RBL-2H3	IC₅₀	0.22 mM Compound: ketotifen fumarate	Inhibition of rat RBL2H3 cell degranulation assessed as inhibition of beta-hexosamidase release after 10 mins by microplate reader assay Inhibition of rat RBL2H3 cell degranulation assessed as inhibition of beta-hexosamidase release after 10 mins by microplate reader assay	[PMID: 12398545]
RBL-2H3	IC₅₀	0.22 mM Compound: Ketotifen fumarate	Inhibition of beta-hexosaminidase in anti-DNP IgE sensitized rat RBL2H3 cells after 10 mins Inhibition of beta-hexosaminidase in anti-DNP IgE sensitized rat RBL2H3 cells after 10 mins	[PMID: 15387643]
RBL-2H3	IC₅₀	158 μM Compound: ketotifen fumarate	Antiallergic activity against antigen-IgE-mediated degranulation in rat RBL2H3 cells assessed as inhibition of DNP-BSA-induced beta-hexosaminidase release preincubated for 10 mins before DNP-BSA challenge measured after 10 mins Antiallergic activity against antigen-IgE-mediated degranulation in rat RBL2H3 cells assessed as inhibition of DNP-BSA-induced beta-hexosaminidase release preincubated for 10 mins before DNP-BSA challenge measured after 10 mins	[PMID: 19414259]
RBL-2H3	IC₅₀	35.2 μM Compound: 6	Inhibition of DNP-BSA-induced degranulation in rat RBL2H3 cells assessed as reduction in beta-hexosaminidase release after 20 mins by spectrophotometry Inhibition of DNP-BSA-induced degranulation in rat RBL2H3 cells assessed as reduction in beta-hexosaminidase release after 20 mins by spectrophotometry	[PMID: 22543029]

In Vitro

Ketotifen (0-100 μM; 2 or 4 days) inhibits SARS-CoV-2 with an EC₅₀ of 48.9 μM; and increases the percentage inhibition of SARS-CoV-2 to 79%, 83% and 93% when co-administers with 25, 50 and 100 μM Indomethacin, respectively^[3].
Ketotifen (0-50 μM; 24 h) has inhibitory activity against PR8, pH1N1 and H3N2 with EC₅₀s of 5.9 μM, 33.7 μM and 48.5 μM, respectively; and exhibits relatively low cytotoxicity in MDCK cells (EC₅₀=291 μM)^[4].

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

In Vivo

Ketotifen (80 mg/kg; i.g.; daily for 3 days) reduces end organ damage and mortality in mice infected with influenza virus^[4].
Ketotifen fumarate (0.4 mg/kg; i.p.; daily for 10 days) reduces encephalomyelitis (EAE) prevalence and severity^[5].

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

Animal Model:

Female C57BL/6 mice (4-6 weeks; intranasal infection with 1×10³ TCID₅₀ of PR8 in 30 μL of DMEM)^[4]
Dosage:

80 mg/kg
Administration:

i.g.; daily for 3 days
Result:

Reduced end organ damage and mortality in infected mice.

Animal Model:

Female C57BL/6 mice (5-6 weeks old; subcutaneously immunized with 150 μg of MOG_35-55 peptide containing 4 mg/mL of Mycobacterium tuberculosis)^[5]
Dosage:

0.4 mg/kg
Administration:

i.p.; daily for 10 days (from the 7th day of infection)
Result:

Reduced EAE prevalence and severity; reduced oxidative stress status and inflammasome activation at the CNS; reduced the amount of T cells, especially Th1, in the CNS; downregulated local mRNA expression for mast cell enzymes and preserves blood-CNS barrier permeability; triggered lymphocyte accumulation in draining lymph nodes.

Chemical Information

CAS No. 34580-14-8
Appearance Solid
Molecular Weight 425.50
Formula C₂₃H₂₃NO₅S
Color White to off-white
SMILES

O=C(C1=C/2C=CS1)CC3=CC=CC=C3C2=C4CCN(C)CC/4.O=C(O)/C=C/C(O)=O
Synonyms

HC 20511 fumarate
Structure Classification
- Others
Initial Source
- Endogenous metabolite
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (3)

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Journal Impact Factor

Eur J Med Chem

Innovative medicinal chemistry strategies for enhancing drug solubility. [Abstract]

2024 Dec 5:279:116842. PMID: 39260319
Cell Oncol (Dordr)

Repurposing ketotifen as a therapeutic strategy for neuroendocrine prostate cancer by targeting the IL-6/STAT3 pathway. [Abstract]

2023 Oct;46(5):1445-1456. PMID: 37120492
Microbiol Spectr

In vitro interaction of naphthoquine with ivermectin, atovaquone, curcumin, and ketotifen in the asexual blood stage of Plasmodium falciparum 3D7. [Abstract]

2024 Jul 2;12(7):e0063024. PMID: 38780257

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (235.02 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 16.67 mg/mL (39.18 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

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

2.3502 mL

11.7509 mL

23.5018 mL

5 mM

0.4700 mL

2.3502 mL

4.7004 mL

10 mM

0.2350 mL

1.1751 mL

2.3502 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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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: ≥ 2.5 mg/mL (5.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: PBS

Solubility: 37.5 mg/mL (88.13 mM); Clear solution; Need ultrasonic

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.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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) .

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 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]. Klooker TK, et al. The mast cell stabiliser ketotifen decreases visceral hypersensitivity and improves intestinal symptoms in patients with irritable bowel syndrome. Gut. 2010 Sep;59(9):1213-21. [Content Brief]

[2]. Zhang H, et al. Advances in the discovery of exosome inhibitors in cancer. J Enzyme Inhib Med Chem. 2020;35(1):1322-1330. [Content Brief]

[3]. Kiani P, et al. In Vitro Assessment of the Antiviral Activity of Ketotifen, Indomethacin and Naproxen, Alone and in Combination, against SARS-CoV-2. Viruses. 2021 Mar 26;13(4):558. [Content Brief]

[4]. Enkirch T, et al. Identification and in vivo Efficacy Assessment of Approved Orally Bioavailable Human Host Protein-Targeting Drugs With Broad Anti-influenza A Activity. Front Immunol. 2019 Jun 5;10:1097. [Content Brief]

[5]. Pinke KH, et al. Calming Down Mast Cells with Ketotifen: A Potential Strategy for Multiple Sclerosis Therapy? Neurotherapeutics. 2020 Jan;17(1):218-234. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	2.3502 mL	11.7509 mL	23.5018 mL	58.7544 mL
	5 mM	0.4700 mL	2.3502 mL	4.7004 mL	11.7509 mL
	10 mM	0.2350 mL	1.1751 mL	2.3502 mL	5.8754 mL
	15 mM	0.1567 mL	0.7834 mL	1.5668 mL	3.9170 mL
	20 mM	0.1175 mL	0.5875 mL	1.1751 mL	2.9377 mL
	25 mM	0.0940 mL	0.4700 mL	0.9401 mL	2.3502 mL
	30 mM	0.0783 mL	0.3917 mL	0.7834 mL	1.9585 mL
DMSO	40 mM	0.0588 mL	0.2938 mL	0.5875 mL	1.4689 mL
	50 mM	0.0470 mL	0.2350 mL	0.4700 mL	1.1751 mL
	60 mM	0.0392 mL	0.1958 mL	0.3917 mL	0.9792 mL
	80 mM	0.0294 mL	0.1469 mL	0.2938 mL	0.7344 mL
	100 mM	0.0235 mL	0.1175 mL	0.2350 mL	0.5875 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Ketotifen fumarate

3 Cited Publications

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Ketotifen fumarate

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Publications Citing Use of MedChemExpress (MCE) Ketotifen fumarate

All Histamine Receptor Isoforms

All Endogenous Metabolite Isoforms

Biological Activity

Chemical Information

Publications (3)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Ketotifen fumarate Related Classifications

HY-B0157A Related Classifications