13246  YM-58483

BTP 2 (CAS 223499-30-7)

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).1 YM-58483 also inhibits lung interleukin-4 and cysteinyl leukotriene generation as well as airway eosinophil infiltration in animal models of asthma.2
1  J. Ishikawa, K. Ohga, T. Yoshino, et al. A pyrazole derivative, YM-58483, potently inhibits store-operated sustained Ca2+ influx and IL-2 production in T lymphocytes. Journal of Immunology 170 4441-4449 (2003).
2  T. Yoshino, J. Ishikawa, K. Ohga, et al. YM-58483, a selective CRAC channel inhibitor, prevents antigen-induced airway eosinophilia and late phase asthmatic responses via Th2 cytokine inhibition in animal models. European Journal of Pharmacology 560 225-233 (2007).

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1 mg €34.00
5 mg €153.00
10 mg €270.00
25 mg €592.00
Pricing updated 2017-01-19.
Prices are subject to change without notice.

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