Ketotifen (Synonyms: HC 20-511)

Name: Ketotifen
Brand: MedChemExpress
SKU: HY-B0157
Rating: 5.0 (3 reviews)

Cat. No.: HY-B0157 Purity: 99.94%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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

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Ketotifen 화학구조

CAS No. : 34580-13-7

사이즈	재고	수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 3 publication(s) in Google Scholar

Other Forms of Ketotifen:

Ketotifen fumarate In-stock
Ketotifen-¹³C,d₃ 견적 받기
Ketotifen-d₃ 견적 받기
Ketotifen (Standard) 견적 받기

3 Publications Citing Use of MCE Ketotifen

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Endogenous Metabolite Isoform Specific Products:

View All Isoforms

Human Endogenous Metabolite Microbial Metabolite

View All Histamine Receptor Isoform Specific Products:

View All Isoforms

H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

Biological Activity
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target

H₁ Receptor

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	1 1 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 1 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]
RBL-2H3	IC₅₀	35.2 3 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]
Sf21	IC₅₀	738.4 3 Compound: Ketotifen	Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]
RBL-2H3	IC₅₀	27.9 3 Compound: Ketotifen	Antiallergic activity in rat RBL-2H3 cell model assessed as inhibition rate of IgE-mediated degranulation in by measuring beta-aminosidase Antiallergic activity in rat RBL-2H3 cell model assessed as inhibition rate of IgE-mediated degranulation in by measuring beta-aminosidase	[PMID: 38640354]
Sf21	IC₅₀	>1 2 Compound: Ketotifen	Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]
RBL-2H3	IC₅₀	35.2 3 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]
Sf21	IC₅₀	738.4 3 Compound: Ketotifen	Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]
Sf21	IC₅₀	> 1000 3 Compound: Ketotifen	Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]

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 (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.

Clinical Trial

분자량

309.43

화학식

C₁₉H₁₉NOS

CAS No.

34580-13-7

Appearance

Solid

Color

Off-white to yellow

SMILES

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

Structure Classification

Others

Initial Source

Endogenous metabolite

선적

Room temperature in continental US; may vary elsewhere.

보관

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

용액&용해도

In Vitro:

DMSO : 10 mg/mL (32.32 mM; ultrasonic and warming and heat to 60°C; 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	3.2317 mL	16.1587 mL	32.3175 mL
5 mM	0.6463 mL	3.2317 mL	6.4635 mL
10 mM	0.3232 mL	1.6159 mL	3.2317 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

몰농도 계산기
농도 희석 계산기

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 mg/mL (3.23 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
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 mg/mL (3.23 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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 mg/mL (3.23 mM); Clear solution

This protocol yields a clear solution of ≥ 1 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 (10.0 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

Animal weight
(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.

순도&문서

Purity: 99.94%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (254 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]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	3.2317 mL	16.1587 mL	32.3175 mL	80.7937 mL
	5 mM	0.6463 mL	3.2317 mL	6.4635 mL	16.1587 mL
	10 mM	0.3232 mL	1.6159 mL	3.2317 mL	8.0794 mL
	15 mM	0.2154 mL	1.0772 mL	2.1545 mL	5.3862 mL
	20 mM	0.1616 mL	0.8079 mL	1.6159 mL	4.0397 mL
	25 mM	0.1293 mL	0.6463 mL	1.2927 mL	3.2317 mL
	30 mM	0.1077 mL	0.5386 mL	1.0772 mL	2.6931 mL

Ketotifen Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
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:

Ketotifen34580-13-7HC 20-511Endogenous MetaboliteHistamine ReceptorSARS-CoVInfluenza VirusSARS coronavirusH1mast cellantiviralPR8pH1N1H3N2encephalomyelitisasthmaInhibitorinhibitorinhibit

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Ketotifen (Synonyms: HC 20-511)

고객리뷰

Other Forms of Ketotifen:

Ketotifen Related Antibodies

3 Publications Citing Use of MCE Ketotifen

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Endogenous Metabolite Isoform Specific Products:

View All Histamine Receptor Isoform Specific Products:

Biological Activity

순도&문서

References

고객리뷰

Ketotifen Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

Ketotifen Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

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