Biological Activity
Blocker of store-operated Ca2+ entry (SOCE), which mediates the activation of non-excitable cells (e.g. lymphocytes). Inhibits calcium release-activated calcium (CRAC) channels; suppresses thapsigargin-induced sustained Ca2+ influx (IC50 = 100 nM). Displays immuno-modulatory and anti-inflammatory effects; suppresses cytokine production and proliferation of T cells in vitro.
Compound Libraries
YM 58483 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 421.32 |
| Formula | C15H9F6N5OS |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 223499-30-7 |
| PubChem ID | 2455 |
| InChI Key | XPRZIORDEVHURQ-UHFFFAOYSA-N |
| Smiles | O=C(C3=C(C)N=NS3)NC1=CC=C(N2N=C(C(F)(F)F)C=C2C(F)(F)F)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.13 | 100 | |
| ethanol | 42.13 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 421.32. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.37 mL | 11.87 mL | 23.73 mL |
| 5 mM | 0.47 mL | 2.37 mL | 4.75 mL |
| 10 mM | 0.24 mL | 1.19 mL | 2.37 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.47 mL |
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References
References are publications that support the products' biological activity.
Ishikawa et al (2003) A pyrazole derivative, YM-58483, potently inhibits store-operated sustained Ca2+ influx and IL-2 production in T lymphocytes. J.Immunol. 170 4441 PMID: 12707319
Zitt et al (2004) Potent inhibition of Ca2+ release-activated Ca2+ channels and T-lymphocyte activation by the pyrazole derivative BTP2. J.Biol.Chem. 26 12427 PMID:
Ohga et al (2008) Characterization of YM-58483/BTP2, a novel store-operated Ca2+ entry blocker, on T cell-mediated immune responses in vivo. Int.Immunopharmocol. 8 1787 PMID:
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