Chemical Name: N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-4-methyl-1,2,3-thiadiazole-5-carboxamide
Biological ActivityBlocker 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
A pyrazole derivative, YM-58483, potently inhibits store-operated sustained Ca2+ influx and IL-2 production in T lymphocytes.
Ishikawa et al.
Potent inhibition of Ca2+ release-activated Ca2+ channels and T-lymphocyte activation by the pyrazole derivative BTP2.
Zitt et al.
Characterization of YM-58483/BTP2, a novel store-operated Ca2+ entry blocker, on T cell-mediated immune responses in vivo.
Ohga et al.
Citations for YM 58483
The citations listed below are publications that use Tocris products. Selected citations for YM 58483 include:
2 Citations: Showing 1 - 2
A store-operated calcium channel inhibitor attenuates collagen-induced arthritis.
Authors: Gao Et al.
Br J Pharmacol 2015;172:2991
Potent analgesic effects of a store-operated calcium channel inhibitor.
Authors: Gao Et al.
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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.