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MCS134380 SEW2871 [256414-75-2]

MCS134380 SEW2871 [256414-75-2]

详情

英文名称 SEW2871
别名 ;5-[4-Phenyl-5-(trifluoromethyl)-2-thienyl]-3-[3-(trifluoromethyl)phenyl]- 1,2,4-oxadiazole
分子式 C20H10F6N2OS
CAS号 256414-75-2
分子量 440.36
MDL MFCD00096600
名称 SEW2871
介绍 >98%评论
属性 存贮条件 储存温度2-8°C

文档信息

文档 COA NMR HPLC MSDS Datasheet

生物活性

描述SEW2871 是高度选择性的,具有口服活性的 S1P1 激动剂,EC50 为 13.8 nM。SEW2871 激活 ERK,Akt 和 Rac 信号通路,并诱导 S1P1 内在化和再循环。SEW2871 减少血液中的淋巴细胞数量,并在糖尿病,阿尔茨海默氏病,肝纤维化和炎症反应方面具有治疗意义。
靶点

EC50: 13.8 nM (S1P1)[2]

参考文献

[1]. Park SJ, et al. Sphingosine 1-Phosphate Receptor Modulators and Drug Discovery. Biomol Ther (Seoul). 2017 Jan 1;25(1):80-90.

[2]. Jo E, et al. S1P1-selective in vivo-active agonists from high-throughput screening: off-the-shelf chemical probes of receptor interactions, signaling, and fate. Chem Biol. 2005 Jun;12(6):703-15.

[3]. Dong J, et al. Oral treatment with SEW2871, a sphingosine-1-phosphate type 1 receptor agonist, ameliorates experimental colitis in interleukin-10 gene deficient mice. Clin Exp Immunol. 2014 Jul;177(1):94-101.

物理化学性质

密度 1.4±0.1 g/cm3
沸点 490.3±55.0 °C at 760 mmHg
熔点 94.5-95.3ºC
分子式 C20H10F6N2OS
分子量 440.362
闪点 250.3±31.5 °C
精确质量 440.041809
PSA 67.16000
LogP 8.42
外观性状 白色固体
蒸汽压 0.0±1.2 mmHg at 25°C
折射率 1.535

文献

[1]Differential activation of receptors and signal pathways upon stimulation by different doses of sphingosine-1-phosphate in endothelial cells.
[2] Pharmacologic targeting of sphingosine-1-phosphate receptor 1 improves the renal microcirculation during sepsis in the mouse.
[3] Sphingosine Kinase 2 and Ceramide Transport as Key Targets of the Natural Flavonoid Luteolin to Induce Apoptosis in Colon Cancer Cells.

英文别名

别名

1,2,4-Oxadiazole, 5-[4-phenyl-5-(trifluoromethyl)-2-thienyl]-3-[3-(trifluoromethyl)phenyl]-

5-[4-Phenyl-5-(trifluoromethyl)-2-thienyl]-3-[3-(trifluoromethyl)phenyl]-1,2,4-oxadiazole

5-[4-phenyl-5-(trifluoromethyl)thiophen-2-yl]-3-[3-(trifluoromethyl)phenyl]-1,2,4-oxadiazole

5-[4-Phenyl-5-(trifluoromethyl)-2-thienyl]-3-[3-(trifluoromethyl)phenyl]- 1,2,4-oxadiazole

5-[4-phenyl-5-(trifluoromethyl)thien-2-yl]-3-[3-(trifluoromethyl)phenyl]-1,2,4-oxadiazole

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