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抑制剂描述:

产品名称:YM-58483 (BTP2)

产品别名:见爱必信官网

英文别名:YM-58483 (BTP2)

靶点:CRAC Channel

CAS:223499-30-7

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

 YM-58483/BTP2是钙池调控钙离子进入(SOCE)的阻滞剂,参与调解不可兴奋细胞如淋巴细胞的激活。

溶解性:DMSO : 78 mg/mL (185.1 mM)
Ethanol : 78 mg/mL (185.1 mM)

体外研究:

YM-58483 (also known as BTP2) is a selective SOCE blocker that inhibits anti-CD3 antibody-induced sustained Ca2+ influx in Jurkat T cells. YM-58483 does not cross-react with voltage-operated Ca2+entry, K+ channels, or Cl? channels. It suppresses the CRAC, TRPC3, and TRPC5 channels, and also facilitates the TRPM4 channel. YM-58483 suppresses cytokine production (IL-2, IL-4, IL-5, IFN-γ, etc.) and proliferation in T cells in vitro. YM-58483 inhibits the spleen cell proliferation associated with MLR by suppressing NF-AT activation via sustained influx of extracellular Ca2+. YM-58483 potently inhibits IL-2 production and NF-AT-driven promoter activity, but not AP-1-driven promoter activity in Jurkat cells.

体内研究:YM-58483 exhibits inhibitory effects on several types of allergic asthma models, such as airway hyperresponsiveness, early and late bronchoconstriction, and antigen-induced airway eosinophilia, with the reduction of IL-4 and leukotriene levels in the airways of rats and guinea pigs. YM-58483 also inhibits the anti-host CTL response, donor T cell expansion, and IFN-γ production in GVHD mice. YM-58483 selectively inhibits storeoperated Ca2+ influx, it does not affect baseline intracellular Ca2+ levels. YM-58483 caused no apparent change in general activity in mice at doses up to 30 mg/kg, p.o.

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