SEW2871 是一种口服有效的、高选择性的S1P1(鞘氨醇 -1- 磷酸 1 型受体)激动剂，其EC50为 13.8 nM。SEW2871 可激活ERK，Akt和Rac信号通路，并诱导 S1P1 内化和循环。SEW2871 可减少血液中的淋巴细胞数量。SEW2871 可用于糖尿病，阿尔茨海默氏病，肝纤维化和炎症的研究。
| 生物活性 | SEW2871 is an orally active, potent, highly selectiveS1P1(sphingosine-1-phosphate type 1 receptor) agonist, with anEC50of 13.8 nM. SEW2871 activatesERK,Akt, andRacsignaling 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[1][2]. |
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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)[2].
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体内研究
(In Vivo) | SEW2871 (20 mg/kg, Gavage, once daily for 2 weeks) ameliorates established experimental colitis in IL-10–/–mice[3].
SEW2871 (0.5 mg/kg, IP, daily for 2 weeks) inhibited β amyloid (Aβ1-42)-induced spatial memory impairment and hippocampal neuronal loss in a rat model of Alzheimer’s disease[2].
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[2].
SEW2871 is effective in protecting kidneys against ischaemia-reperfusion injury by reducing CD4+T cell infiltration in mice[3].
| Animal Model: | IL-10–/–(interleukin (IL)-10 gene-deficient) mice, a murine model of Crohn's disease (CD)[3] | | 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 CD4+CD45+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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(56.77 mM;Need ultrasonic) 配制储备液 | 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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. 请依序添加每种溶剂： 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。 2. 请依序添加每种溶剂： 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。 *以上所有助溶剂都可在本网站选购。
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