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Biological Activity for YM 58483
YM 58483 is a 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 for YM 58483
Technical Data for YM 58483
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for YM 58483
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for YM 58483
The following data is based on the product molecular weight 421.32. Batch specific molecular weights may vary from batch to batch due to the degree 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|
References for YM 58483
References are publications that support the biological activity of the product.
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
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
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Keywords: YM 58483, YM 58483 supplier, YM58483, inhibitor, inhibits, CRAC, SOCE, store-operated, channel, calcium, Ca2+, release, activated, entry, channels, inhibitors, Btp2, Other, Calcium, Channels, General, Signaling, Agents, STIM-Orai, 3939, Tocris Bioscience
2 Citations for YM 58483
Citations are publications that use Tocris products. Selected citations for YM 58483 include:
Gao et al (2013) Potent analgesic effects of a store-operated calcium channel inhibitor. Pain 154 2034 PMID: 23778292
Gao et al (2015) A store-operated calcium channel inhibitor attenuates collagen-induced arthritis. Br J Pharmacol 172 2991 PMID: 25651822
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Reviews for YM 58483
Average Rating: 4 (Based on 3 Reviews.)
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YM 58483 was used to study the role of the MRGPRX2 receptor in store-operated calcium entry using human mast cells (LAD2 cells). At a concentration of 0.3 and 1 uM of YM58483 inhibited the calcium entry induced by cortistatin in mast cells.
HEK293 cells were incubated with intracellular Ca2+ sensitive dye, Fura-2AM in normal tyrode solution for 40 min, washed and kept aside for 20 min. Fura2-loaded cells were excited alternately at 340 and 380 nm and fluorescence at 510 nm was expressed as 340/380 ratio. Intracellular Ca2+ stores were depleted with 30 μM BHQ which promotes store-operated Ca2+ entry into the cells upon addition of 1 mM extracellular Ca2+. Preincubation of cells with 10 μM BTP2 (YM 58483) for 10 min attenuates this Ca2+ entry.
Used to block SOCE mechanism but no effect was seen. Unsure about efficacy of the compound, it might be a lack of SOCE involvement in the biological process studied here.