YM 58483

Name: YM 58483
Brand: Tocris Bioscience
SKU: 3939
Rating: 4 (3 reviews)

Tocris Bioscience a Bio-Techne Brand

Catalog # 3939

Citations (2)

(3)

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Key Product Details

Description:	Inhibitor of SOCE in non-excitable cells
Alternative Names:	Btp2
Chemical Name:	N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-4-methyl-1,2,3-thiadiazole-5-carboxamide
Purity:	≥99% (HPLC)
Molecular Weight:	421.32

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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

YM 58483 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for YM 58483

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for YM 58483

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	42.13	100
	ethanol	42.13	100

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

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References for YM 58483

References are publications that support the biological activity of the product.

Ohga Characterization of YM-58483/BTP2, a novel store-operated Ca²⁺ entry blocker, on T cell-mediated immune responses in vivo. Int.Immunopharmocol. 2008 PMID: 18793756
Zitt Potent inhibition of Ca²⁺ release-activated Ca²⁺ channels and T-lymphocyte activation by the pyrazole derivative BTP2. J.Biol.Chem. 2004 PMID: 14718545
Ishikawa A pyrazole derivative, YM-58483, potently inhibits store-operated sustained Ca²⁺ influx and IL-2 production in T lymphocytes. J.Immunol. 2003 PMID: 12707319

Citations for YM 58483 (2)

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Citations are publications that use Bio-Techne products. Selected citations for YM 58483 include:

Gao et al. (2015) A store-operated calcium channel inhibitor attenuates collagen-induced arthritis. Br J Pharmacol. 172:2991
PMID: 25651822
Gao et al. (2013) Potent analgesic effects of a store-operated calcium channel inhibitor. Pain. 154:2034
PMID: 23778292

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Customer Reviews for YM 58483 (3)

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Inhibits calcium entry in mast cells.

Name: ANANTH KUMAR KAMMALA

Species: Human

Assay Type: In Vitro

Cell Line/Tissue: LAD2 - mast cells

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.

PMID: 32038646 Reference
BTP2 attenuates store-operated Ca2+ entry

Name: Anonymous

Species: Human

Assay Type: In Vitro

Cell Line/Tissue: HEK293

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.
Store-operated calcium entry blocker

Name: Anonymous

Species: Mouse

Assay Type: Ex Vivo

Cell Line/Tissue: Brain slice

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.

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Product Documents for YM 58483

COA

Certificate of Analysis

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