Ex26 (S1P1-IN-Ex26) 是一种强效和选择性的sphingosine 1-phosphate receptor 1(S1P1) 拮抗剂 (IC50=0.93 nM)，对 S1P1的选择性大于其他 Sphingosine 1-phosphate receptor 约 3,000 倍。Ex26 可用于实验性自身免疫性脑脊髓炎的研究。
| 生物活性 | Ex26 (S1P1-IN-Ex26) is a potent and selectivesphingosine 1-phosphate receptor 1(S1P1) antagonist (IC50=0.93 nM). Ex26 shows >3,000-fold selectivity for S1P1over other Sphingosine 1-phosphate receptors. Ex26 can be used in experimental autoimmune encephalomyelitis reseach[1]. |
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体外研究
(In Vitro) | Ex26 (0-10 μM; 1 h) treatment shows excellent selectivity for S1P1over other Sphingosine 1-phosphate receptors[1].
Cell Viability Assay[1] | Cell Line: | U2OS cells, and Chinese hamster ovary cells | | Concentration: | 0-10 μM | | Incubation Time: | 1 hour | | Result: | Confirmed a potent and selective antagonist of S1P1(IC50=0.93 nM). |
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体内研究
(In Vivo) | Ex26 (i.p.; 3 mg/kg; once daily; 3 d) treatment disrupts S1P1signaling inhibiting the lymphocyte and thymocyte egress[1].
Ex26 (i.p.; 30 mg/kg; once daily; 15 d) treatment alleviates experimental autoimmune encephalomyelitis by S1P1antagonism[1].
| Animal Model: | Eight-week-old male C57Bl/6J mice[1] | | Dosage: | 3 mg/kg | | Administration: | Intraperitoneal injection; 3 mg/kg; once daily; 3 days | | Result: | Induced lymphocyte sequestration at low doses, possessing an ED50of 0.06 mg/kg after 2 hours treatment. Led to significant retention of T and B cells within the lymph nodes and significant decreases in T and B cells within the spleen. |
| Animal Model: | Eight-week-old male C57Bl/6J mice induced with experimental autoimmune encephalomyelitis[1] | | Dosage: | 30 mg/kg | | Administration: | Intraperitoneal injection; 30 mg/kg; once daily; 15 days | | Result: | Inhibited both lymphocyte infiltration and destruction of the white matter in the spinal cord of mice euthanized at the end of the experiment. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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