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N,N''-1,4-丁烷二基双[N'-(3-异异硫氰基苯基)硫脲

用途

MRS2578是P2Y6受体拮抗剂,IC50为37 nM,对P2Y1,P2Y2,P2Y4和P2Y11受体的抑制性较弱。

名称

[ CAS 号 ]:
711019-86-2

[ 中文名 ]:
N,N''-1,4-丁烷二基双[N'-(3-异异硫氰基苯基)硫脲

[ 英文名 ]:
MRS 2578

[英文别名 ]:

MRS 2578
MRS2578

生物活性

[ 描述 ]:

MRS2578是P2Y6受体拮抗剂,IC50为37 nM,对P2Y1,P2Y2,P2Y4和P2Y11受体的抑制性较弱。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> P2Y受体

研究领域 >> 心血管疾病

[参考文献]

[1]. Mamedova LK, et al. Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors. Biochem Pharmacol, 2004, 67(9), 1763-1770.

[2]. Riegel AK, et al. Selective induction of endothelial P2Y6 nucleotide receptor promotes vascular inflammation. Blood, 2011, 117(8), 2548-2555.

[3]. Vieira RP, et al. Purinergic receptor type 6 contributes to airway inflammation and remodeling in experimental allergic airway inflammation. Am J Respir Crit Care Med, 2011, 184(2), 215-223.

[相关活性小分子]

物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
652.7±65.0 °C at 760 mmHg

[ 分子式 ]:
C₂₀H₂₀N₆S₄

[ 分子量 ]:
472.673

[ 闪点 ]:
348.5±34.3 °C

[ 精确质量 ]:
472.063232

[ PSA ]:
201.20000

[ LogP ]:
5.10

[ 外观性状 ]:
白色固体

[ 蒸汽压 ]:
0.0±2.0 mmHg at 25°C

[ 折射率 ]:
1.687

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
DMSO: ~17 mg/mL

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 符号 ]:

GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H312 + H332-H315-H319-H334-H335

[ 警示性声明 ]:
P261-P284-P301 + P310 + P330-P302 + P352 + P312-P304 + P340 + P312-P342 + P311

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
20/21/22-36/37/38-42

[ 安全声明 (欧洲) ]:
22-26-36/37/39-45

[ 危险品运输编码 ]:
UN 2811

[ WGK德国 ]:
3

文献

Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors.

Biochem. Pharmacol. 67 , 1763-1770, (2004)

The physiological role of the P2Y(6) nucleotide receptor may involve cardiovascular, immune and digestive functions based on the receptor tissue distribution, and selective antagonists for this recept...

Activated microglia cause reversible apoptosis of pheochromocytoma cells, inducing their cell death by phagocytosis.

J. Cell Sci. 129 , 65-79, (2016)

Some apoptotic processes, such as phosphatidylserine exposure, are potentially reversible and do not necessarily lead to cell death. However, phosphatidylserine exposure can induce phagocytosis of a c...

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