YM 58483

立即咨询

YM 58483

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

223499-30-7

包装与价格：

包装	价格(元)
10mg	电议
50mg	电议

产品介绍

化学性质

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	421.32
Cas No.	223499-30-7
Formula	C₁₅H₉F₆N₅OS
Solubility	insoluble in H2O; ≥50 mg/mL in EtOH; ≥90 mg/mL in DMSO
Chemical Name	N-(4-(3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)-4-methyl-1,2,3-thiadiazole-5-carboxamide
Canonical SMILES	FC(F)(C1=CC(C(F)(F)F)=NN1C(C=C2)=CC=C2NC(C3=C(C)N=NS3)=O)F
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

YM 58483, also known as BTP2, is a SOCE blocker. SOCE has been found in macrophages, basophils, dendritic cells, and mast cells as well as T cells. The SOCE-related channels include the Ca²⁺release-activated Ca²⁺(CRAC) channel which is a highly Ca²⁺-selective channel, and the non-selective, Ca²⁺-permeable transient receptor potential (TRP) channels, which regulate the activation of non-excitable cells such as lymphocytes. YM 58483 has been reported to inhibit cytokine production and proliferation in T cells, and may serve as a potential medicinal candidate for treatment of bronchial asthma.

References:

1. Ohga K, Takezawa R, Arakida Y, et al. Characterization of YM-58483/BTP2, a novel store-operated Ca²⁺entry blocker, on T cell-mediated immune responses in vivo. International Immunopharmacology, 2008, 8(13-14): 1787-1792.

2. Ishikawa J, Ohga K, Yoshino T, et al. A pyrazole derivative, YM-58483, potently inhibits store-operated sustained²⁺influx and IL-2 production in T lymphocytes. Journal of Immunology, 2003, 170(9): 4441-4449.

试验操作

Cell experiment:[2]
Cell lines	Jurkat cells
Reaction Conditions	0.0003 ~ 1 μM YM 58483
Applications	YM 58483 dose-dependently inhibited PHA-induced IL-2 production in Jurkat cells, with an IC50 value of 17 ± 3.2 nM. Moreover, YM 58483 potently inhibited NF-AT-driven promoter activity, but not AP-1-driven promoter activity in Jurkat cells.
Animal experiment:[1]
Animal models	Mouse graft-versus-host disease (GVHD) model
Dosage form	1 ~ 30 mg/kg Once daily by oral route (p.o.) for 10 days
Applications	YM 58483 (1 ~ 30 mg/kg, p.o.) and cyclosporine A (1 ~ 30 mg/kg, p.o.) inhibited donor anti-host cytotoxic T lymphocyte (CTL) activity and IFN-γ production, and also reduced the number of donor T cells, especially donor CD⁸⁺T cells, in the spleen.
Note	The technical data provided above is for reference only.
	References: 1. Ohga K, Takezawa R, Arakida Y, et al. Characterization of YM-58483/BTP2, a novel store-operated Ca²⁺entry blocker, on T cell-mediated immune responses in vivo. International Immunopharmacology, 2008, 8(13-14): 1787-1792. 2. Ishikawa J, Ohga K, Yoshino T, et al. A pyrazole derivative, YM-58483, potently inhibits store-operated sustained²⁺influx and IL-2 production in T lymphocytes. Journal of Immunology, 2003, 170(9): 4441-4449.