Biological Activity
ym 58483, also known as btp2, is a soce blocker. soce has been found in macrophages, basophils, dendritic cells, and mast cells as well as t cells. the soce-related channels include the ca2+ release-activated ca2+ (crac) channel which is a highly ca2+-selective channel, and the non-selective, ca2+-permeable transient receptor potential (trp) channels, which regulate the activation of non-excitable cells such as lymphocytes. ym 58483 has been reported to inhibit cytokine production and proliferation in t cells, and may serve as a potential medicinal candidate for treatment of bronchial asthma.1. ohga k, takezawa r, arakida y, et al. characterization of ym-58483/btp2, a novel store-operated ca2+ entry blocker, on t cell-mediated immune responses in vivo. international immunopharmacology, 2008, 8(13-14): 1787-1792.2. ishikawa j, ohga k, yoshino t, et al. a pyrazole derivative, ym-58483, potently inhibits store-operated sustained ca2+ influx and il-2 production in t lymphocytes. journal of immunology, 2003, 170(9): 4441-4449.
Biochem/physiol Actions
YM-58483 is a selective Ca++ release-activated Ca++ (CRAC) [a.k.a. store-operated Ca++ (SOC) channels] that mediate Ca++ influx in T cells and other inflammatory cells. CRAC channel inhibitors have potential clinical applications in autoimmune disease, transplant rejection, allergic airway inflammation and bronchial asthma. YM-58483 is also promoted as a tool for CRAC studies; may be used as a gold standard.
