Ketotifen free base · Synonyms: HC 20-511

Ketotifen (HC 20-511) is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer.

For research use only. Not for human or veterinary use.

Target Endogenous Metabolite Histamine Receptor SARS-CoV Influenza Virus

Research area InfectionInflammation/Immunology Endocrinology

Purity >98% Stock Inquire

Data Sheet SDS COA

Ketotifen structure

CAS No.: 34580-13-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
500 mg	USD 450.00	BP-02178-500mg	In stock	Get quote
1 g	USD 720.00	BP-02178-1g	In stock	Get quote
2 g	USD 1,150.00	BP-02178-2g	In stock	Get quote
3 g	USD 1,380.00	BP-02178-3g	In stock	Get quote
5 g	USD 1,840.00	BP-02178-5g	In stock	Get quote
10 g	USD 2,950.00	BP-02178-10g	In stock	Get quote

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Description

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 .

Biological activity

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

Identifiers

SMILES: O=C(C1=C/2C=CS1)CC3=CC=CC=C3C2=C4CCN(C)CC/4
InChIKey: ZCVMWBYGMWKGHF-UHFFFAOYSA-N

Specifications

MW (average): 309.4250
Formula: C₁₉H₁₉NOS
CAS No.: 34580-13-7
Physical state: Solid
Color: Off-white to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃, 3 years; 4℃, 2 years; In solvent -20℃, 1 month;

Solubility

soluble in DMSO

Documents

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.

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

[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.

[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.

[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.

Same target

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Same research area

Search InfectionInflammation/Immunology