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Icanbelimod

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Chemical Structure| 1514888-56-2 同义名 : S1p receptor agonist 1
CAS号 : 1514888-56-2
货号 : A723833
分子式 : C23H24FN3O3
纯度 : 98%
分子量 : 409.45
MDL号 : MFCD30738002
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：
生物活性
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].
实验方案
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
参考文献

[1]Li Z, Chen W, Hale JJ, Lynch CL, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Chrebet G, Parent SA, Bergstrom J, Card D, Forrest M, Quackenbush EJ, Wickham LA, Vargas H, Evans RM, Rosen H, Mandala S. Discovery of potent 3,5-diphenyl-1,2,4-oxadiazole sphingosine-1-phosphate-1 (S1P1) receptor agonists with exceptional selectivity against S1P2 and S1P3. J Med Chem. 2005 Oct 6;48(20):6169-73.