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YM-58483

SKU: orb1303957

Description

YM-58483 (BTP2) is a potent and selective CRAC channel inhibitor that effectively suppresses store-operated calcium entry (SOCE) and downstream calcium signaling. This tool compound is widely used in both in vitro and in vivo research to investigate immune cell activation, T-cell proliferation, and mast cell degranulation.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Images & Validation

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YM-58483

Key Properties

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CAS Number223499-30-7
MW421.32
Purity99.33%
FormulaC15H9F6N5OS
SMILESCc1nnsc1C(=O)Nc1ccc(cc1)-n1nc(cc1C(F)(F)F)C(F)(F)F
TargetCalcium Channel
SolubilityEthanol:78 mg/mL (185.13 mM);DMSO:250 mg/mL (593.37 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.75 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

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In Vivo
As a selective SOCE inhibitor, YM-58483 inhibits sustained calcium ion influx induced by anti-CD3 antibodies in Jurkat T cells. It inhibits CRAC, TRPC3, and TRPC5 channels, while promoting the TRPM4 channel, leading to the suppression of cytokine production (IL-2, IL-4, IL-5, IFN-γ, etc.) and T-cell proliferation. YM-58483 impedes the proliferation of splenocytes related to MLR by inhibiting the activation of NF-AT. Additionally, it significantly suppresses the production of IL-2 and the promoter activity driven by NF-AT, without affecting the AP-1-driven promoter activity within Jurkat cells.
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In Vitro
In various models of allergic asthma, including airway hyperresponsiveness, early and late-phase bronchoconstriction, and antigen-induced airway eosinophilia, YM-58483 demonstrates inhibitory effects. Furthermore, in rat and guinea pig tissues, it reduces levels of leukotrienes and IL-4. In mice with GVHD, YM-58483 also suppresses host-versus-graft CTL reactions, donor T cell proliferation, and the production of IFN-γ. Notably, YM-58483 (30 mg/kg, p.o.) does not significantly affect general activity in mice .
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Cell Research
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. (Only for Reference)
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Storage & Handling

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StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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Ca2+ release-activated Ca2+ channels, Calcium release-activated channels, Calcium Channel, BTP 2, BTP2, BTP-2, CalciumChannel, CRAC Channel, CRAC channel, Inhibitor, inhibit, YM 58483, YM58483, YM-58483

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  • YM-58483

    YM-58483 [orb1225616]

    >98% (HPLC)

    223499-30-7

    421.3203

    C15H9F6N5OS

    2 mg, 5 mg, 100 mg, 50 mg, 1 g, 500 mg, 200 mg, 25 mg, 10 mg
Quality Guarantee

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Compound Identifiers

PubChem CID
2455 ↗

Key Properties

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No computed properties available.

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YM-58483 (orb1303957)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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1 mg
$ 70.00
2 mg
$ 90.00
1 ml x 10 mM (in DMSO)
$ 110.00
5 mg
$ 110.00
10 mg
$ 160.00
25 mg
$ 280.00
50 mg
$ 450.00
100 mg
$ 630.00
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