SEW2871 is a potent and selective sphingosine-1-phosphate 1 (S1P1) receptor agonist. Activates S1P1 receptor with an EC50 of 13 nM, but does not activate S1P2, S1P3, S1P4 or S1P5 receptors at concentrations up to 10 μM. Cell-permeable and active in vivo.
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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] |
Dose | Rat: 5 mg/kg[3] (i.p.) Mice: 1.25 mg/kg - 30 mg/kg/d[2] (p.o.), 40 mg/kg[4] (p.o.) |
Administration | i.p., p.o. |
计算器 | ||||
存储液制备 | ![]() |
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 |
CAS号 | 256414-75-2 |
分子式 | C20H10F6N2OS |
分子量 | 440.36 |
SMILES Code | FC(C1=CC(C2=NOC(C3=CC(C4=CC=CC=C4)=C(C(F)(F)F)S3)=N2)=CC=C1)(F)F |
MDL No. | MFCD00096600 |
别名 | |
运输 | 蓝冰 |
InChI Key | OYMNPJXKQVTQTR-UHFFFAOYSA-N |
Pubchem ID | 4077460 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, sealed in dry, 2-8°C |
溶解方案 |
请根据您的动物给药指南选择适当的溶解方案。 以下溶解方案都请先按照体外实验的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
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