货号:A723833 同义名: S1p receptor agonist 1
Icanbelimod是一种 S1P 受体激动剂,具有诱导 S1P1 内化的作用 (EC50 = 9.83 nM),适用于关节炎和实验性自身免疫性脑炎 (EAE) 的研究,具有潜在的免疫调节作用。
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描述 | Sphingosine-1-phosphate (S1P) is a metabolic product of sphingolipid and it activates five G protein-coupled receptors, S1P1-5. S1P-agonist-1 has been identified as a potent S1P1 receptor agonist with an IC50 value of 0.6nM. It shows less affinity for S1P4 and S1P5 with IC50 values of 70 and 1.0nM, respectively. The IC50 value for S1P3 is 12μM. The half-lives (t1/2) of S1P-agonist-1 in rats was 8.5h. The minimal single dose of S1P-agonist-1 required for the maximal sequestration of peripheral blood lymphocytes (PBL) was 10, 0.5, and 0.5mg/kg (p.o.) in mice, rats, and dogs, respectively. The pharmacodynamic ED50 for S1P-agonist-1 in the PBL lowering response assay was 0.03mpk (p.o.). In a rat skin allograft model, the combined treatment of S1P-agonist-1 (5.0mpk p.o. per day, 28 days) and CsA (1mpk/day, i.p.) showed the median graft survival times of 22 days[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.44mL 0.49mL 0.24mL |
12.21mL 2.44mL 1.22mL |
24.42mL 4.88mL 2.44mL |
CAS号 | 1514888-56-2 |
分子式 | C23H24FN3O3 |
分子量 | 409.45 |
别名 | S1p receptor agonist 1 |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 5 mg/mL(12.21 mM),配合低频超声,并水浴加热至45℃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 |