Home GPCR & G Protein S1P Receptor modulator Ozanimod For research use only.

Ozanimod

Synonyms: RPC1063

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

Ozanimod Chemical Structure

Ozanimod Chemical Structure

CAS: 1306760-87-1

Selleck's Ozanimod has been cited by 6 publications

Purity & Quality Control

Batch: Purity: 99.97%
99.97

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Biological Activity

Description Ozanimod 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 vitro

In S1P1R-HEK293T cells, Ozanimod induces sustained S1P1R internalization and degradation. [1]
Kinase Assay In vitro pharmacology assays
Cell signaling assays used the LiveBLAzer-FRET B/G assay to detect cAMP (S1P1R) or β-arrestin signaling (S1P4R). Assays are performed in 384-well plates in triplicate according to manufacturer directions. Compound stocks are stored at 10 mM in 100% DMSO at -80°C, and initially diluted 1:10 with 20% (2-hydoxypropyl)-β-cyclodextrin. A 10-point dose response curve is generated at 40-times the final assay concentration in 10 mM Hepes pH 7.4, containing 0.1% Pluronic F-127. For the S1P1R assay, 80 μM forskolin is included in the diluent. Briefly, 104 cells/well are incubated with a dose response of ligand at 37°C for 4 hrs. CC4-AM substrate and probenecid are added and incubated at 37°C for a further 2 hrs and analyzed with a SpectramaxM5. For S1P1R cAMP assays, data is normalized to the maximum fluorescence generated by 2 μM forskolin. For GTPγS binding assays, 1-5μg/well of membrane protein is incubated with 10 μM GDP, 100-500 μg/well Wheat Germ Agglutinin PVT SPA beads in 50 mM HEPES, 100 mM NaCl, 10 mM MgCl2, 20 μg/ml saponin and 0.1% fatty acid free BSA for 15 minutes in 96-well plates. After the addition of compound and 200 pM GTP [35S] 1250Ci/mmol), the plates are incubated for 120 minutes and centrifuged at 300g for 5 minutes. Radioactivity is detected with a TopCount Instrument. All data is fit with a four parameter variable slope non-linear regression (GraphPad Prism) to generate half-maximal effective concentration (EC50) and maximum efficacy relative to S1P.
Cell Research Cell lines HEK293T cells
Concentrations 1 μM
Incubation Time 1 h
Method

Cells expressing S1P1 receptors were incubated with vehicle control or 1 μM RPC1063 for 1 h.
In Vivo
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]
Animal Research 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
Dosages 0.1-3 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06188637 Not yet recruiting Ulcerative Colitis Geert D''Haens|Bristol-Myers Squibb|Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA) March 1 2024 Phase 4
NCT05470985 Recruiting Crohn Disease Bristol-Myers Squibb August 22 2023 Phase 2|Phase 3
NCT05811416 Recruiting Relapsing-remitting Multiple Sclerosis (RRMS) Bristol-Myers Squibb June 14 2023 --
NCT05777902 Recruiting Multiple Sclerosis I.R.C.C.S. Fondazione Santa Lucia January 31 2023 Phase 4
NCT05076175 Recruiting Colitis Ulcerative Bristol-Myers Squibb May 30 2022 Phase 2|Phase 3

Chemical lnformation & Solubility

Molecular Weight 404.46 Formula

C23H24N4O3
CAS No. 1306760-87-1 SDF Download Ozanimod SDF
Smiles CC(C)OC1=C(C=C(C=C1)C2=NC(=NO2)C3=C4CCC(C4=CC=C3)NCCO)C#N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 40 mg/mL ( (98.89 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble


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In vivo
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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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