Ozanimod (RPC1063) - 98%, high purity , CAS No.1306760-87-1, Agonist of S1P 1 receptor;Agonist of S1P 2 receptor;Agonist of S1P 3 receptor;Agonist of S1P 4 receptor;Agonist of S1P 5 receptor
Ozanimod (RPC1063) - 98%, high purity , CAS No.1306760-87-1, Agonist of S1P 1 receptor;Agonist of S1P 2 receptor;Agonist of S1P 3 receptor;Agonist of S1P 4 receptor;Agonist of S1P 5 receptor
In S1P1R-HEK293T cells, Ozanimod induces sustained S1P1R internalization and degradation.
In vivo
Ozanimod shows high oral bioavailability and volume of distribution. In a MOG-induced EAE mouse model, Ozanimod (3 mg/kg, p.o.) suppresses clinical symptoms. In a rat TNBS model of inflammatory bowel disease, Ozanimod (1.2 mg/kg, p.o.) inhibits clinical and histological disease scores. In a Naïve CD4+CD45Rbhi T cell adoptive transfer model, Ozanimod (1.2 mg/kg, p.o.) also significantly reduced disease severity as assessed by measuring the degree of inflammation, gland loss, hyperplasia, neutrophil infiltrate and mucosal thickness.
1.Scott FL, Clemons B, Brooks J, Brahmachary E, Powell R, Dedman H, Desale HG, Timony GA, Martinborough E, Rosen H et al.. (2016) Ozanimod (RPC1063) is a potent sphingosine-1-phosphate receptor-1 (S1P1 ) and receptor-5 (S1P5 ) agonist with autoimmune disease-modifying activity.. Br J Pharmacol, 173 (11):(1778-92). [PMID:26990079]
2.Taylor Meadows KR, Steinberg MW, Clemons B, Stokes ME, Opiteck GJ, Peach R, Scott FL. (2018) Ozanimod (RPC1063), a selective S1PR1 and S1PR5 modulator, reduces chronic inflammation and alleviates kidney pathology in murine systemic lupus erythematosus.. PLoS ONE, 13 (4):(e0193236). [PMID:29608575]
3.Derfuss T, Mehling M, Papadopoulou A, Bar-Or A, Cohen JA, Kappos L. (2020) Advances in oral immunomodulating therapies in relapsing multiple sclerosis.. Lancet Neurol, 19 (4):(336-347). [PMID:32059809]
4.Argollo M, Furfaro F, Gilardi D, Roda G, Allocca M, Peyrin-Biroulet L, Danese S. (2020) Modulation of sphingosine-1-phosphate in ulcerative colitis.. Expert Opin Biol Ther, 20 (4):(413-420). [PMID:32093531]
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