Ketotifen (fumarate)

Ketotifen is a histamine H1 receptor antagonist (Ki = 1.3 nM) and mast cell stabilizer. It is selective for H1 receptors over H2 and H3 receptors (Kis = 987 and 2,500 nM, respectively). Ketotifen (50 and 100 µM) inhibits degranulation of rat peritoneal mast cells induced by compound 48/80 (Cay-22173). It inhibits the passive cutaneous anaphylaxis (PCA) reaction in rats by 54.6% when administered orally at a dose of 20 mg/kg. Ketotifen (30 mg/kg) inhibits the quick phase airway response in a rat ovalbumin-induced immediate airway response model. Formulations containing ketotifen have been used in the treatment of itching associated with allergic conjunctivitis.Formal Name: 4,9-dihydro-4-(1-methyl-4-piperidinylidene)-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one-(2E)-2-butenedioate. CAS Number: 34580-14-8. Synonyms: HC 20511. Molecular Formula: C19H19NOS . C4H4O4. Formula Weight: 425.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/mL, DMSO: 25 mg/mL, DMSO:PBS(pH 7.2) (1:2): .3 mg/mL, Ethanol: .5 mg/mL. lambdamax: 250, 309 nm. SMILES: O=C1C2=C(C=CS2)/C(C3=CC=CC=C3C1)=C4CCN(C)CC/4.OC(/C=C/C(O)=O)=O. InChi Code: InChI=1S/C19H19NOS.C4H4O4/c1-20-9-6-13(7-10-20)18-15-5-3-2-4-14(15)12-17(21)19-16(18)8-11-22-19,5-3(6)1-2-4(7)8/h2-5,8,11H,6-7,9-10,12H2,1H3,1-2H,(H,5,6)(H,7,8)/b,2-1+. InChi Key: YNQQEYBLVYAWNX-WLHGVMLRSA-N.