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CAS No.: 256414-75-2

SEW2871 Catalog No. CSN10124

Synonyms: SEW2871

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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靶点选择性

生物活性

实验方案

技术信息

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]
动物研究
剂量
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.)

给药途径
i.p., p.o.
参考文献

动物研究
剂量	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.)
给药途径	i.p., p.o.

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2709 mL
- 11.3543 mL
- 22.7086 mL
- 5 mM
- 0.4542 mL
- 2.2709 mL
- 4.5417 mL
- 10 mM
- 0.2271 mL
- 1.1354 mL
- 2.2709 mL

技术信息

CAS号

256414-75-2

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H10F6N2OS

运输

蓝冰

分子量

440.36

别名

SEW2871

溶解度

DMSO	30.0 mg/mL (68.1 mM) warming

动物实验配方

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SEW2871 Catalog No. CSN10124

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