Home Transmembrane Transporters Calcium Channel inhibitor YM-58483 (BTP2)

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YM-58483 (BTP2) Calcium Channel inhibitor

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) Calcium Channel inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 421.32

Purity & Quality Control

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

Related Products

Signaling Pathway

Calcium Channel Signaling Pathways

Calcium Channel Signaling Pathway

Mechanism of Action

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. It does not cross-react with voltage-operated Ca²⁺ entry, K⁺ channels, or Cl⁻ channels. This compound suppresses the CRAC, TRPC3, and TRPC5 channels, and also facilitates the TRPM4 channel. It 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]. It 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 concentrations of YM-58483 (BTP2) for 30 min at 37°C. After treatment with this compound, the cells were stimulated with 1 μM ionomycin for 30 min at 37°C. Following stimulation, the cells were centrifuged at 200×g for 2 min and 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 (BTP2) 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. It also inhibits the anti-host CTL response, donor T cell expansion, and IFN-γ production in GVHD mice. This compound selectively inhibits storeoperated Ca2+ influx, it does not affect baseline intracellular Ca2+ levels. It 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.

References
  • https://pubmed.ncbi.nlm.nih.gov/18793756/
  • https://pubmed.ncbi.nlm.nih.gov/12707319/

Chemical Information

Molecular Weight 421.32 Formula

C15H9F6N5OS
CAS No. 223499-30-7 SDF Download SDF
Synonyms N/A
Smiles CC1=C(SN=N1)C(=O)NC2=CC=C(C=C2)N3C(=CC(=N3)C(F)(F)F)C(F)(F)F

Storage and Stability

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.

Handling Instructions

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