5-[4-苯基-5-(三氟甲基)-2-噻吩基]-3-[3-(三氟甲基)苯基]-1,2,4-恶二唑

用途

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。

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名称

[ CAS 号 ]:
256414-75-2

[ 中文名 ]:
5-[4-苯基-5-(三氟甲基)-2-噻吩]-3-[3-(三氟甲基)苯基]-1,2,4-噁二唑

[ 英文名 ]:
SEW2871

[中文别名 ]:

[英文别名 ]:

生物活性

[ 描述 ]:

[ 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

[ 储存条件 ]:
2-8°C，避光干燥密封

安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H300

[ 警示性声明 ]:
P264-P301 + P310

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
25

[ 安全声明 (欧洲) ]:
45

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

文献

Differential activation of receptors and signal pathways upon stimulation by different doses of sphingosine-1-phosphate in endothelial cells.

Exp. Physiol. 100(1) , 95-107, (2015)

What is the central question of this study? Why do different doses of sphingosine-1-phosphate (S1P) induce distinct biological effects in endothelial cells? What is the main finding and its importance...

Pharmacologic targeting of sphingosine-1-phosphate receptor 1 improves the renal microcirculation during sepsis in the mouse.

J. Pharmacol. Exp. Ther. 352(1) , 61-6, (2014)

Microvascular failure is hallmark of sepsis in humans and is recognized as a strong predictor of mortality. In the mouse subjected to cecal ligation and puncture (CLP) to induce a clinically relevant ...

Sphingosine Kinase 2 and Ceramide Transport as Key Targets of the Natural Flavonoid Luteolin to Induce Apoptosis in Colon Cancer Cells.

PLoS ONE 10 , e0143384, (2015)

The plant flavonoid luteolin exhibits different biological effects, including anticancer properties. Little is known on the molecular mechanisms underlying its actions in colorectal cancer (CRC). Here...

更多文献

5-[4-苯基-5-(三氟甲基)-2-噻吩基]-3-[3-(三氟甲基)苯基]-1,2,4-恶二唑

用途

名称

生物活性

物理化学性质

安全信息

文献

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