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

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

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

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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

Mechanism of Action

Targets/IC50/Ki
SOCE
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+. It 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 (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..
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