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Description: Ozanimod (also known as RPC1063) is a potent, selective and orally bioavailable S1P Receptor 1 modulator. Ozanimod is useful in the treatment of S1P1-associated diseases. The EC50 values of Ozanimod were 160 +/- 60 pM and 410 +/- 160 pM for S1P1 receptors in the inhibition of cAMP generation and35S-GTPgammaS binding. The 83% Emax value of ozanimod against S1P5 receptor was 11 +/- 4.3 nM. RPC1063 dose-dependently decreased S1P1 receptor re-expression on the cell surface and resulted in near complete and sustained loss of cell surface receptor expression at concentrations above 10 nM in S1P1 receptor-HEK293T cells.
References: Br J Pharmacol. 2016 Jun; 173(11):1778-92.
Chemical Name: (S)-5-(3-(1-((2-hydroxyethyl)amino)-2, 3-dihydro-1H-inden-4-yl)-1, 2, 4-oxadiazol-5-yl)-2-isopropoxybenzonitrile
InChi Key: XRVDGNKRPOAQTN-FQEVSTJZSA-N
InChi Code: InChI=1S/C23H24N4O3/c1-14(2)29-21-9-6-15(12-16(21)13-24)23-26-22(27-30-23)19-5-3-4-18-17(19)7-8-20(18)25-10-11-28/h3-6, 9, 12, 14, 20, 25, 28H, 7-8, 10-11H2, 1-2H3/t20-/m0/s1
SMILES Code: N#CC1=CC(C2=NC(C3=CC=CC4=C3CC[CH]4NCCO)=NO2)=CC=C1OC(C)C
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