For research use only.
CAS No. 223499-30-7
YM-58483/BTP2 is a blocker of store-operated Ca2+ entry (SOCE), which regulates the activation of non-excitable cells such as lymphocytes.
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Choose Selective Calcium Channel Inhibitors
|Description||YM-58483/BTP2 is a blocker of store-operated Ca2+ entry (SOCE), which regulates the activation of non-excitable cells such as lymphocytes.|
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.
|In vivo||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.|
|In vitro||DMSO||84 mg/mL (199.37 mM)|
|Ethanol||84 mg/mL (199.37 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% CMC Na
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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