Potent and selective S1P1 receptor antagonist (IC50 = 0.93 nM). Exhibits > 3,000-fold selectivity for S1P1 over S1P2, S1P3, S1P4 and S1P5. Induces lymphocyte sequestration in peripheral lymph nodes and upregulates S1P1 receptor expression. Reduces disease severity in mice with EAE. Increases IFN-α production in stimulated dendritic cells in vivo.
Teijaro et al (2016) S1PR1-mediated IFNAR1 degradation modulates plasmacytoid dendritic cell IF.-a autoamplification. Proc.Natl.Acad.Sci.U.S.A. 113 1351 PMID:26787880 |Cahalan et al (2013) Sphingosine 1-phosphate receptor 1 (S1P1) upregulation and amelioration of experimental autoimmune encephalomyelitis by an S1P1 antagonist. Mol.Pharmacol. 83 316 PMID:23204443 |Kleinwort et al (2018) S1P signalling differentially affects migration of peritoneal B cell populations in vitro and influences the production of intestinal IgA in vivo. Int.J.Mol.Sci. 19 E391 PMID:29382132