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MedChemExpress - Model Ketotifen fumarate - 34580-14-8

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[1][2][3][4].

Ketotifen fumarate

MCE China：Ketotifen fumarate

Brand：MedChemExpress (MCE)

Cat. No.HY-B0157A

CAS：34580-14-8

Synonyms：HC 20511 fumarate

Purity：99.92%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

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].

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].

IC50 & Target：H1 Receptor

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]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
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