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      Ozanimod (RPC1063)
      Ozanimod (RPC1063)

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      This product is for research use only, not for human use. We do not sell to patients.
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      InvivoChem Cat #: V1507
      CAS #: 1306760-87-1Purity ≥98%

      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 and[35S]-GTPγS 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.

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      Molecular Weight (MW)404.46
      FormulaC23H24N4O3
      CAS No.1306760-87-1
      Storage-20℃ for 3 years in powder form
      -80℃ for 2 years in solvent
      Solubility (In vitro)DMSO: 81 mg/mL (200.3 mM)
      Water: <1 mg/mL
      Ethanol: 10 mg/mL (24.7 mM)
      Other info

      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[[email protected]@H]4NCCO)=NO2)=CC=C1OC(C)C           

      SynonymsRPC1063; RPC-1063; RPC 1063


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      In Vitro

      In vitro activity: In S1P1R-HEK293T cells, Ozanimod induces sustained S1P1R internalization and degradation.

      Kinase Assay: Ozanimod is a potent and selective S1P1 and S1P5 receptor agonist with EC50s of 410±160 pM and 11±4.3 nM in [35S]-GTPγS binding, respectively. 

      Cell Assay: Ozanimod(RPC1063) was a specific agonist for S1P1 and S1P5 receptors. The EC50values were 160 ± 60 pM and 410 ± 160 pM for S1P1 receptors in the inhibition of cAMP generation and[35S]-GTPγS 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 after 1 h incubation.

      In VivoIn 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.
      Animal modelMOG-induced EAE model in C57Bl6 mice, TNBS model of inflammatory bowel disease in male Sprague Dawley rats, and Naive CD4+CD45Rbhi T cell adoptive transfer model in SCID mice
      Formulation & DosageDissolved in 5% DMSO, 5% Tween-20, 90% 0.1N HCl; 0.1-3 mg/kg; oral givage 
      References

      Br J Pharmacol. 2016 Jun;173(11):1778-92

      These protocols are for reference only. InvivoChem does not independently validate these methods.

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