YM-58483

Calcium release-activated calcium (CRAC) channels mediate sustained calcium influx in electrically non-excitable cells. CRAC channels are activated by the release of calcium from intracellular stores, as induced by inositol trisphosphate. CRAC channel activation is essential for the activation of leukocytes and the production of cytokines and inflammatory mediators. YM-58483 is a potent inhibitor of CRAC channels, blocking thapsigargin-induced sustained calcium influx, Th2 cytokine production, and NF-AT-driven promoter activity in T lymphocytes (IC50 = 100 nM). YM-58483 also inhibits lung interleukin-4 and cysteinyl leukotriene generation as well as airway eosinophil infiltration in animal models of asthma.Formal Name: N-[4-[3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-4-methyl-1,2,3-thiadiazole-5-carboxamide. CAS Number: 223499-30-7. Synonyms: BTP 2. Molecular Formula: C15H9F6N5OS. Formula Weight: 421.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 10 mg/ml. lambdamax: 275 nm. SMILES: O=C(C1=C(C)N=NS1)NC2=CC=C(N3N=C(C(F)(F)F)C=C3C(F)(F)F)C=C2. InChi Code: InChI=1S/C15H9F6N5OS/c1-7-12(28-25-23-7)13(27)22-8-2-4-9(5-3-8)26-11(15(19,20)21)6-10(24-26)14(16,17)18/h2-6H,1H3,(H,22,27). InChi Key: XPRZIORDEVHURQ-UHFFFAOYSA-N.