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SEW2871

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Chemical Structure| 256414-75-2 同义名 : SEW​2871
CAS号 : 256414-75-2
货号 : A656270
分子式 : C20H10F6N2OS
纯度 : 99%+
分子量 : 440.362
MDL号 : MFCD00096600
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(56.77 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 SEW2871 is a specific and potent agonist of S1P1 receptor with IC50 value of 37nM for displacement of S1P, with much higher affinity to S1P1 receptor versus IC50 values >4600nM for S1P2-5[1]. SEW2871 is structurally unrelated to S1P but with similar effect of S1P. It selectively activated the binding of S1P1 receptor to GTP with EC50 value of 13nM in GTPγS binding assays. Treatment with 100nM SEW2871 led to calcium flux stimulation on the murine S1P receptors. Also it stimulated the phosphorylation of AKT and ERK1 signals in S1P1-CHO cells at concentration ranging in 5-500nM, as well as increased cell migration at concentration of 1μM. Oral administration of SEW2871 at 10mg/kg induced lymphatic clearance in mesenteric lymph nodes[2].
作用机制 SEW2871 can mimic the effect of S1P.[1][2]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.27mL

0.45mL

0.23mL

11.35mL

2.27mL

1.14mL

22.71mL

4.54mL

2.27mL
参考文献

[1]Hale JJ, Lynch CL, et al. A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists. J Med Chem. 2004 Dec 30;47(27):6662-5.

[2]Sanna MG, Liao J, et al. Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate. J Biol Chem. 2004 Apr 2;279(14):13839-48. Epub 2004 Jan 19.