| Description |
Ex26 (S1P1-IN-Ex26) is a potent and selective Sphingosine 1-phosphate receptor 1 (S1P1) antagonist (IC50=0.93 nM). Ex26 shows >3,000-fold selectivity for S1P1 over other Sphingosine 1-phosphate receptors. Ex26 can be used in experimental autoimmune encephalomyelitis reseach[1].
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| Related Catalog |
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| Target |
IC50: 0.93 nM (S1P1)[1]
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| In Vitro |
Ex26 (0-10 μM; 1 h) treatment shows excellent selectivity for S1P1 over 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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| In Vivo |
Ex26 (i.p.; 3 mg/kg; once daily; 3 d) treatment disrupts S1P1 signaling inhibiting the lymphocyte and thymocyte egress[1]. Ex26 (i.p.; 30 mg/kg; once daily; 15 d) treatment alleviates experimental autoimmune encephalomyelitis by S1P1 antagonism[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 ED50 of 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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| References |
[1]. Stuart M Cahalan, et al. Sphingosine 1-phosphate receptor 1 (S1P(1)) upregulation and amelioration of experimental autoimmune encephalomyelitis by an S1P(1) antagonist. Mol Pharmacol. 2013 Feb;83(2):316-21.
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