Ex26

Research use only, not for human use.

Ex26 (S1P1-IN-Ex26) is a selective and potent sphingosine 1-phosphate receptor 1 (S1P1) antagonist that disrupts SR-B1-S1PR1 interactions and inhibits S1P-S1PR1 signaling.

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.

Ex26 (0-10 μM; 1 h) treatment shows excellent selectivity for S1P1 over other Sphingosine 1-phosphate receptors.Cell Viability Assay 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).

Ex26 (i.p.; 3 mg/kg; once daily; 3 d) treatment disrupts S1P1 signaling inhibiting the lymphocyte and thymocyte egress.Ex26 (i.p.; 30 mg/kg; once daily; 15 d) treatment alleviates experimental autoimmune encephalomyelitis by S1P1 antagonism.Animal Model:Eight-week-old male C57Bl/6J mice 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 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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GPCR/G Protein

S1P Receptor

S1P Receptor

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1233332-37-0

494.99

C28H28ClFN2O3

>98% (HPLC)

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O=C(O)C1(NC(=O)C2=C(C=C(C=C2C)C=3C=C(C=CC3F)NC(C4=CC=C(Cl)C(=C4)C)C)C)CC1

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(-20℃)

With Ice Pack

≥ 2 years