Ozanimod (RPC1063)

Catalog No.S7952

Ozanimod (RPC1063) Chemical Structure

Molecular Weight(MW): 404.46

Ozanimod (RPC1063) is a selective oral S1P Receptor 1 modulator. Phase 3.

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Biological Activity

Description Ozanimod (RPC1063) is a selective oral S1P Receptor 1 modulator. Phase 3.
Targets
S1P1R [1]
(Cell-free assay)
S1P5R [1]
(Cell-free assay)
0.41 nM(EC50) 11 nM(EC50)
In vitro

In S1P1R-HEK293T cells, Ozanimod induces sustained S1P1R internalization and degradation. [1]

In vivo 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]

Protocol

Animal Research:[1]
- Collapse
  • Animal Models: MOG-induced EAE model in C57Bl6 mice, TNBS model of inflammatory bowel disease in male Sprague Dawley rats, and Na飗e CD4+CD45Rbhi T cell adoptive transfer model in SCID mice
  • Formulation: 5% DMSO, 5% Tween-20, 90% 0.1N HCl
  • Dosages: 0.1-3 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 81 mg/mL (200.26 mM)
Ethanol 10 mg/mL (24.72 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 404.46
Formula

C23H24N4O3

CAS No. 1306760-87-1
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03464097 Recruiting Drug: Ozanimod|Other: Placebo Crohn Disease Celgene June 27 2018 Phase 3
NCT03440385 Recruiting Drug: Ozanimod|Other: Placebo Crohn Disease Celgene March 7 2018 Phase 3
NCT03440372 Recruiting Drug: Ozanimod|Other: Placebo Crohn Disease Celgene February 27 2018 Phase 3
NCT02994381 Completed Drug: RPC1063 Healthy Volunteers Celgene October 2016 Phase 1
NCT02531126 Recruiting Drug: RPC1063 Ulcerative Colitis Celgene December 2 2015 Phase 3
NCT02576717 Active not recruiting Drug: RPC1063 Multiple Sclerosis Celgene October 16 2015 Phase 3

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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S1P Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID