YM 58483

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

Cat. No. 3939 10 篇引用文献 3 条评论提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

Pricing	Availability		Qty

说明： Inhibitor of SOCE in non-excitable cells

别名： Btp2

化学名： N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-4-methyl-1,2,3-thiadiazole-5-carboxamide

纯度： ≥99% (HPLC)

说明书

引用文献 (10)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 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.

化合物库 for YM 58483

YM 58483 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。

技术数据 for YM 58483

分子量	421.32
公式	C₁₅H₉F₆N₅OS
储存	Store at +4°C
纯度	≥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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

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

溶解性数据 for YM 58483

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	DMSO	42.13	100
	ethanol	42.13	100

制备储备液 for YM 58483

以下数据基于产品分子量 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.

浓度/溶剂体积/质量	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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产品说明书 for YM 58483

分析证书/产品说明书

化学品安全技术说明书

参考文献 for YM 58483

参考文献是支持产品生物活性的出版物。

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: 14718545

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: 18793756

If you know of a relevant reference for YM 58483, please let us know.

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关键词: 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

10 篇 YM 58483 的引用文献

引用文献是使用了 Tocris 产品的出版物。 YM 58483 的部分引用包括：

Faten et al (2021) Targeting CAMKK2 and SOC Channels as a Novel Therapeutic Approach for Sensitizing Acute Promyelocytic Leukemia Cells to All-Trans Retinoic Acid. Cells 10 PMID: 34943872

Olivier et al (2021) TRAIL Triggers CRAC-Dependent Calcium Influx and Apoptosis through the Recruitment of Autophagy Proteins to Death-Inducing Signaling Complex. Cells 11 PMID: 35011619

Robert J et al (2021) PAR-2-activated secretion by airway gland serous cells: role for CFTR and inhibition by Pseudomonas aeruginosa. Am J Physiol Lung Cell Mol Physiol 320 L845-L879 PMID: 33655758

Silvia et al (2021) RGS10 physically and functionally interacts with STIM2 and requires store-operated calcium entry to regulate pro-inflammatory gene expression in microglia. Cell Signal 83 109974 PMID: 33705894

Gao et al (2015) A store-operated calcium channel inhibitor attenuates collagen-induced arthritis. Br J Pharmacol 172 2991 PMID: 25651822

Martin et al (2017) Molecular Phenotyping Combines Molecular Information, Biological Relevance, and Patient Data to Improve Productivity of Early Drug Discovery. Cell Chem Biol 24 624-634.e3 PMID: 28434878

Gao et al (2013) Potent analgesic effects of a store-operated calcium channel inhibitor. Pain 154 2034 PMID: 23778292

Yanfeng et al (2022) Enhanced Orai1-mediated store-operated Ca2+ channel/calpain signaling contributes to high glucose-induced podocyte injury. J Biol Chem 298 101990 PMID: 35490782

Jeremy et al (2020) Calcium-stimulated disassembly of focal adhesions mediated by an ORP3/IQSec1 complex. Elife 9 PMID: 32234213

Gregory R et al (2020) Distinct pharmacological profiles of ORAI1, ORAI2, and ORAI3 channels. Cell Calcium 91 102281 PMID: 32896813

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YM 58483 的评论

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Inhibits calcium entry in mast cells..

By ANANTH KUMAR KAMMALA on 01/30/2021

分析类型： In Vitro

种属： Human

细胞系/组织： 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 参考文献

BTP2 attenuates store-operated Ca2+ entry.

By Anonymous on 07/10/2019

分析类型： In Vitro

种属： Human

细胞系/组织： 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.

By Anonymous on 01/31/2018

分析类型： Ex Vivo

种属： Mouse

细胞系/组织： 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.