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

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YM-58483 (BTP2) Calcium Channel inhibitor

Cat.No.S8380

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

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 421.32 Formula

C15H9F6N5OS

 Storage (From the date of receipt)
CAS No. 223499-30-7 Download SDF Storage of Stock Solutions

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

Solubility

In vitro
Batch:

DMSO : 84 mg/mL (199.37 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 42 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
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. 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].
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 store-operated Ca²⁺ influx and 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].
References

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