SEW 2871|256414-75-2|-陌孚医药/Medlife

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SEW 2871

目录号: PC11220 纯度: ≥98%

CAS No. :256414-75-2

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中文名称

SEW 2871

中文别名

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;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;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

英文名称

SEW 2871

英文别名

5-(4-Phenyl-5-(trifluoromethyl)thiophen-2-yl)-3-(3-(trifluoromethyl)phenyl)-1,2,4-oxadiazole;SEW 2871;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)-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;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;SEW2871;S1P1 Receptor Agonist, SEW2871;Sphingosine-1-Phosphate1 Receptor S1P1 Agonist;5-(4-Phenyl-5-trifluoromethylthiophen-2-yl)-3-(3-trifluoromethylphenyl)-(1,2,4)-ox

Cas No.

256414-75-2

分子式

C₂₀H₁₀F₆N₂Os

分子量

440.36

包装储存

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

SEW2871 is an orally active, potent, highly selective S1P1 (sphingosine-1-phosphate type 1 receptor) agonist, with an EC₅₀ of 13.8 nM. SEW2871 activates ERK, Akt, and Rac signaling pathways and induces S1P1 internalization and recycling. SEW2871 reduces lymphocyte numbers in blood. SEW2871 can be used for the research of diabetes, Alzheimer’s disease, liver fibrosis, and inflammatory responses.

性状

Solid

IC50 & Target[1][2]

S1PR1

13.8 nM (EC₅₀)

体外研究(In Vitro)

SEW2871 exerts a powerful migratory effect by increasing smooth muscle α-actin, procollagen αI and αIII, and total hydroxyproline contents in LX-2 cells (a human hepatic stellate cell line).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

SEW2871 (20 mg/kg, Gavage, once daily for 2 weeks) ameliorates established experimental colitis in IL-10 mice.
SEW2871 (0.5 mg/kg, IP, daily for 2 weeks) inhibited β amyloid (Aβ_1-42)-induced spatial memory impairment and hippocampal neuronal loss in a rat model of Alzheimer’s disease.
SEW2871 (0-0.3 mg/kg, IV) attenuates LPS-induced acute inflammatory lung injury, produces dose-dependent alveolar and vascular barrier protection in C57Bl/6 mice.
SEW2871 is effective in protecting kidneys against ischaemia-reperfusion injury by reducing CD4 T cell infiltration in mice.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	IL-10 (interleukin (IL)-10 gene-deficient) mice, a murine model of Crohns disease (CD)
Dosage:	20 mg/kg
Administration:	Gavage, once daily for 2 weeks
Result:	Ameliorated established colitis in IL-10 mice, associated with a reduction of serum amyloid A concentration, a decreased colon MPO concentration, a depletion of the peripheral CD4CD45 T cells and a reduction of the homing of T cells into colon LP. Suppressed typical cytokines of T helper type 1 (Th1) and Th17 cells and p-STAT-3 expression, and significantly decreased TNF-α, IFN-γ, IL-1β and IL-17A mRNA levels.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

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. [Information]

[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. [Information]

[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. [Information]

溶解度数据

体外研究:

DMSO : 25 mg/mL (56.77 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2709 mL	11.3543 mL	22.7087 mL
5 mM	0.4542 mL	2.2709 mL	4.5417 mL
10 mM	0.2271 mL	1.1354 mL	2.2709 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.72 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.72 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.72 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.72 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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