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- 规格参数
- 包装参数
Biochem/physiol Actions
Ceralifimod (ONO-4641) is an orally active, potent, S1P1 & S1P5 subtype-selective sphingosine-1-phosphate (S1P) receptor agonist (rat S1P1 Ki = 0.772 nM, human S1P5/1/4 Ki = 0.574/0.626/28.2 nM, hS1P2/3 Ki >5.45 μM against S1P by binding assays) that suppresses forskolin-stimulated cAMP accumulation (IC50 = 27.3 pM/hS1P1, 28.64 pM/rS1P1, 334 pM/hS1P5 using respective transfectants) and induces S1P1 downregulation with a higher potency than SEW2871 & S1P (EC50 = 0.778, 118, 132 nM, respectively). Ceralifimod decreases peripheral blood lymphocytes (EDmax 100 μg/kg po.) in rats, and shows in vivo efficacy in rat and murine EAE models (30 & 100 μg/kg/day po.).
Orally active, potent, S1P1 & S1P5 subtype-selective sphingosine-1-phosphate (S1P) receptor agonist with in vivo efficacy in rat and murine EAE models.
Disclaimer
Hygroscopic
| Quality Segment | 100 |
| assay | ≥95% (HPLC) |
| form | powder |
| storage condition | desiccated |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | -10 to -25°C |
| SMILES string | N4(CC(C4)C(=O)O)CC1=C(c2c(cc(cc2)OCc3c(cc(cc3)CCC)OC)CC1)C |
| InChI | 1S/C27H33NO4/c1-4-5-19-6-7-22(26(12-19)31-3)17-32-24-10-11-25-18(2)21(9-8-20(25)13-24)14-28-15-23(16-28)27(29)30/h6-7,10-13,23H,4-5,8-9,14-17H2,1-3H3,(H,29,30) |
| InChI key | QDDQIPUKAXBMBX-UHFFFAOYSA-N |
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