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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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
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Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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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 | 440.362 |
别名 | SEW2871 |
运输 | 蓝冰 |
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 |