Home Transmembrane Transporters Calcium Channel inhibitor YM-58483 (BTP2) For research use only.

YM-58483 (BTP2)

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 (BTP2) Chemical Structure

YM-58483 (BTP2) Chemical Structure

CAS No. 223499-30-7

Purity & Quality Control

Batch: S838001 DMSO]84 mg/mL]false]Ethanol]42 mg/mL]false]Water]Insoluble]false Purity: 99.9%
99.9

YM-58483 (BTP2) Related Products

Signaling Pathway

Calcium Channel Signaling Pathways

Calcium Channel Signaling Pathway

Biological Activity

Description YM-58483/BTP2 is a blocker of store-operated Ca2+ entry (SOCE), which regulates the activation of non-excitable cells such as lymphocytes.
Targets
SOCE [1]
In vitro
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+[1]. YM-58483 potently inhibits IL-2 production and NF-AT-driven promoter activity, but not AP-1-driven promoter activity in Jurkat cells[2].
Cell Research Cell lines Jurkat cells
Concentrations 0.03-3 μM
Incubation Time 30 min
Method

Jurkat cells (1×107 cells/ml) were tested with varying concentration of compounds for 30 min at 37°C. The cells were stimulated with 1 μM ionomycin for 30 min at 37°C. After stimulation, the cells were centrifuged at 200×g for 2 min, and were solubilized in 100 μl of Triton X-100 lysis buffer. The cell lysate was centrifuged at 15,000×g for 20 min; the clarified lysate was subjected to SDS-PAGE; and NF-ATc2 was detected by Western blotting with anti-NF-ATc2 mAb.
In Vivo
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[1].
Animal Research Animal Models Male C57BL/6, BDF1((C57BL/6×DBA2)F1), DBA2 and Balb/c mice
Dosages 1-30 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 421.32 Formula

C15H9F6N5OS
CAS No. 223499-30-7 SDF Download YM-58483 (BTP2) SDF
Smiles CC1=C(SN=N1)C(=O)NC2=CC=C(C=C2)N3C(=CC(=N3)C(F)(F)F)C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 84 mg/mL ( (199.37 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 42 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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