[CAS NO. 223499-30-7] YM-58483 (BTP2)
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PRODUCTS SPECIFICATIONS [223499-30-7]
Store
Catalog
SLK-S8380
Brand
Selleck
CAS
223499-30-7
DESCRIPTION [223499-30-7]
Overview
| MDL | MFCD00220976 |
|---|---|
| Molecular Weight | 421.32 |
| Molecular Formula | C15H9F6N5OS |
| SMILES | O=C(C1=C(C)N=NS1)NC2=CC=C(N3N=C(C(F)(F)F)C=C3C(F)(F)F)C=C2 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3735 mL | 11.8675 mL | 23.7349 mL |
| 5 mM | 0.4747 mL | 2.3735 mL | 4.7470 mL |
| 10 mM | 0.2373 mL | 1.1867 mL | 2.3735 mL |
| 50 mM | 0.0475 mL | 0.2373 mL | 0.4747 mL |
Description
YM-58483/BTP2 is a blocker of (SOCE), which regulates the activation of non-excitable cells such as lymphocytes.
Targets
| SOCE [1] |
In vitro
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.
References
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