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抑制剂/激动剂
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CRAC通道
Calcium Channel
/ YM-58483

YM-58483 {[allProObj[0].p_purity_real_show]}

货号：A172938 同义名： BTP2

YM-58483 是一种选择性的钙释放活化钙通道（CRAC）抑制剂，对 Orai1 具有高亲和力，IC50 值为 10 nM。YM-58483 具有免疫调节和抗炎作用，可用于自身免疫性疾病和炎症相关疾病的研究。

YM-58483 化学结构 CAS号：223499-30-7
YM-58483 化学结构
CAS号：223499-30-7
YM-58483 3D分子结构
CAS号：223499-30-7
YM-58483 化学结构 CAS号：223499-30-7
YM-58483 3D分子结构 CAS号：223499-30-7
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YM-58483 纯度/质量文件 产品仅供科研

货号：A172938 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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更多 >
产品名称 Ca2+ channel-like protein ↓ Calcium Channel ↓ Cav 2.2 ↓ 其他靶点 纯度
CDC25B-IN-2 ✔ Akt 99%+
Clevidipine ✔ 97%
Verapamil HCl ✔ 99%
Amlodipine ✔ 99%
Amlodipine maleate ✔ 98%
(+)-cis-Diltiazem HCl ✔ 95%
Zegocractin ++

Orai1/STIM1-mediated Ca2+ currents, IC50: 120 nM

 		99%+
Tanshinone IIA sulfonate sodium ✔ 98%
Ulixacaltamide ++

hCaV3.1, IC50: 50 nM

hCaV3.2, IC50: 110 nM

 		99%+
Dronedarone Hydrochloride ✔ 95%
Nitrendipine +

Calcium channel, IC50: 95 nM

 		98%
Efonidipine HCl monoethanolate ✔ 98%
Cinnarizine ✔ 98%
SEA0400 ++

NCX, IC50: 33 nM

 		ROS,p38 MAPK,ERK 99%+
Fasudil HCl ✔ Rho,PKA 98%
ML-9 ✔ MLCK,Akt 99%+
Flunarizine 2HCl +

Calcium channel, Ki: 68 nM

 		95%
Lomerizine 2HCl ✔ 98%
Efonidipine ✔ 98%
Levamlodipine ✔ 97%
Nisoldipine ++

L-type Cav1.2, IC50: 10 nM

 		97%
Isradipine ✔ 98%
Lacidipine ✔ 98%
Lercanidipine ✔ 98%
Loureirin B ✔ Potassium Channel 99%+
Tetracaine HCl ✔ 98%
Manidipine +++

Calcium channel, IC50: 2.6 nM

 		98%
Manidipine Dihydrochlorid +++

Calcium channel, IC50: 2.6 nM

 		98%
Nicardipine ✔ 98%
Wilforgine ✔ 98+%
Econazole ✔ 99%+
Ginsenoside Rd ✔ NF-κB 98%
Fendiline HCl ✔ 98+%
Mesaconitine ✔ 98%
Tetrandrine ✔ 95%
Nifedipine ✔ 95%
Nilvadipine ++++

Calcium channel, IC50: 0.03 nM

 		98%
Barnidipine ++++

[3H]nitrendipine, Ki: 0.21 nM

 		95+%
Azelnidipine ✔ 97%
Levetiracetam ✔ 98%
Nimodipine ✔ 95%
Benidipine HCl ✔ 98%
Pinaverium bromide ✔ 98%
Pranidipine ✔ 98%
NP118809 +

N-type Ca2+ channel, IC50: 0.11 μM

L-type calcium channel, IC50: 12.2 μM

 		98%
Amlodipine Besylate +++

Calcium channel, IC50: 1.9 nM

 		97%
Cilnidipine ✔ 98%
Cinepazide Maleate ✔ 98%
Terfenadine ✔ 98%
YM-58483 ✔ 99%+
Ranolazine ✔ 98%
Praeruptorin A ✔ p38 MAPK,Akt 98%
Ranolazine 2HCl ✔ 98%
Felodipine ++++

L-type calcium channel, IC50: 0.15 nM

 		98%
PD173212 +++

N-type Ca2+ channel, IC50: 36 nM

 		98%
Levamlodipine besylate ✔ 97%
Carboxyamidotriazole Orotate ✔ 98%
IGS-1.76 ✔ 98+%
WH-4-023 ++++

Cav 2.2, IC50: 0.001 μM

 		++++

Cav 2.2, IC50: 0.001 μM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

YM-58483 生物活性

靶点

  • Calcium Channel
描述 YM-58483 (BTP2), a pyrazole derivative, potently inhibits Ca(2+) release-activated Ca(2+) (CRAC) channels and interleukin (IL)-2 production in T cells. YM-58483 inhibited IL-4 and IL-5 production in a conalbumine-stimulated murine Th2 T cell clone (D10.G4.1), and IL-5 production in phytohemagglutinin-stimulated human whole blood cells with IC50 values comparable to those reported for its CRAC channel inhibition (around 100 nM). YM-58483 inhibited antigen-induced eosinophil infiltration into airways, and decreased IL-4 and cysteinyl-leukotrienes content in inflammatory airways induced in actively sensitized Brown Norway rats[3]. Intrathecal YM-58483 at the concentration of 300 μM (1.5 nmol) and 1000 μM (10 nmol) produced a significant central analgesic effect on the SNL (spinal nerve ligation) rats, compared with control + vehicle[4]. In the mouse graft-versus-host disease model, YM-58483 (1-30 mg/kg, p.o.) and cyclosporine A (1-30 mg/kg, p.o.) inhibited donor anti-host cytotoxic T lymphocyte activity and IFN-gamma production, and also reduced the number of donor T cells, especially donor CD8+ T cells, in the spleen. YM-58483 and cyclosporine A inhibited T cell proliferation in a one-way mixed lymphocyte reaction (MLR) with IC50 values of 330 and 12.7 nM, respectively. Additionally, YM-58483 (1-10 mg/kg, p.o.) and cyclosporine A (2, 10 mg/kg, p.o.) inhibited the sheep red blood cell (SRBC)-induced delayed type hypersensitivity response[5].

YM-58483 参考文献

[1]Ohga K, Takezawa R, et al. Characterization of YM-58483/BTP2, a novel store-operated Ca2+ entry blocker, on T cell-mediated immune responses in vivo. Int Immunopharmacol. 2008 Dec 20;8(13-14):1787-92.

[2]Ishikawa J, Ohga K, et al. A pyrazole derivative, YM-58483, potently inhibits store-operated sustained Ca2+ influx and IL-2 production in T lymphocytes. J Immunol. 2003 May 1;170(9):4441-9.

[3]Yoshino T, Ishikawa J, Ohga K, Morokata T, Takezawa R, Morio H, Okada Y, Honda K, Yamada T. YM-58483, a selective CRAC channel inhibitor, prevents antigen-induced airway eosinophilia and late phase asthmatic responses via Th2 cytokine inhibition in animal models. Eur J Pharmacol. 2007 Apr 10;560(2-3):225-33

[4]Qi Z, Wang Y, Zhou H, Liang N, Yang L, Liu L, Zhang W. The Central Analgesic Mechanism of YM-58483 in Attenuating Neuropathic Pain in Rats. Cell Mol Neurobiol. 2016 Oct;36(7):1035-43

[5]Ohga K, Takezawa R, Arakida Y, Shimizu Y, Ishikawa J. Characterization of YM-58483/BTP2, a novel store-operated Ca2+ entry blocker, on T cell-mediated immune responses in vivo. Int Immunopharmacol. 2008 Dec 20;8(13-14):1787-92

YM-58483 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.37mL

0.47mL

0.24mL

11.87mL

2.37mL

1.19mL

23.73mL

4.75mL

2.37mL

YM-58483 技术信息

CAS号223499-30-7
分子式C15H9F6N5OS
分子量 421.32
别名 BTP2
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

DMSO: 120 mg/mL(284.82 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

1% CMC Na+water 30 mg/mL suspension

Tags: YM-58483 | 223499-30-7 | BTP2 | YM58483 | YM 58483 | BTP 2 | BTP-2 | Membrane Transporter/Ion Channel | CRAC Channel | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | YM-58483 纯度/质量文件 | YM-58483 亚型比较 | YM-58483 生物活性 | YM-58483 参考文献 | YM-58483 实验方案 | YM-58483 技术信息

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