Ozanimod

Catalog No.S7952 Batch:S795201

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Technical Data

Formula

C23H24N4O3
Molecular Weight 404.46 CAS No. 1306760-87-1
Solubility (25°C)* In vitro DMSO 40 mg/mL (98.89 mM)
Ethanol 10 mg/mL (24.72 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO Corn oil
2.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 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 (from reference)

Kinase Assay:

[1]
  • 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 Assay:

[1]
  • 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.
Animal Study:

[1]
  • 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.

Selleck's Ozanimod has been cited by 6 publications

Ponesimod inhibits astrocyte-mediated neuroinflammation and protects against cingulum demyelination via S1P1 -selective modulation [ FASEB J, 2022, 36(2):e22132] PubMed: 34986275
Role and Mechanism of Ozanimod (RPC1063) in Oligodendrocyte Precursor Cell Differentiation [ China Biotechnology, 2020, (6): 10-19] PubMed: None
Inhibition of histone deacetylase 1 (HDAC1) and HDAC2 enhances CRISPR/Cas9 genome editing. [ Nucleic Acids Res, 2019, 10.1093/nar/gkz1136] PubMed: 31799598
Sphingosine-1-phosphate signalling drives an angiogenic transcriptional programme in diffuse large B cell lymphoma [ Leukemia, 2019, 10.1038/s41375-019-0478-9] PubMed: 31097785
S1PR1 drives a feedforward signalling loop to regulate BATF3 and the transcriptional programme of Hodgkin lymphoma cells [ Leukemia, 2019, 10.1038/s41375-019-0511-z] PubMed: 28878352
The Establishment and Validation of the Human U937 Cell Line as a Cellular Model to Screen Immunomodulatory Agents Regulating Cytokine Release Induced by Influenza Virus Infection [ Virol Sin, 2019, 34(6):648-661] PubMed: 31286365

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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