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Submit ReviewOzanimod is a potent and selective sphingosine-1-phosphate receptor 1 (S1P1) and 5 (S1P5) agonist (EC50 values are 0.41 and 11 nM, respectively, in a [35S]-GTPγS assay). Ozanimod exhibits 27-fold selectivity over S1P5, and >10,000-fold selectivity over S1P2-4. In vitro, Ozanimod induces sustained S1P1 receptor internalization and degradation in S1P1 receptor-HEK293T cells. In vivo, Ozanimod reduces inflammation and disease parameters in rat models of autoimmune disease. Ozanimod reduces chronic inflammation and alleviates kidney pathology in a murine model of systemic lupus erythematosus. Ozanimod is orally bioavailable.
Ozanimod is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 404.46 |
Formula | C23H24N4O3 |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 1306760-87-1 |
PubChem ID | 52938427 |
InChI Key | XRVDGNKRPOAQTN-FQEVSTJZSA-N |
Smiles | N(CCO)[C@@H]1C=2C(=C(C=CC2)C=3N=C(ON3)C4=CC(C#N)=C(OC(C)C)C=C4)CC1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 40.45 | 100 |
The following data is based on the product molecular weight 404.46. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.47 mL | 12.36 mL | 24.72 mL |
5 mM | 0.49 mL | 2.47 mL | 4.94 mL |
10 mM | 0.25 mL | 1.24 mL | 2.47 mL |
50 mM | 0.05 mL | 0.25 mL | 0.49 mL |
References are publications that support the biological activity of the product.
Scott et al (2016) Ozanimod (RPC1063) is a potent sphingosine-1-phosphate receptor-1 (S1P1) and receptor-5 (S1P5) agonist with autoimmune diseasemodifying activity. Br.J.Pharmacol. 173 1778 PMID: 26990079
Selkirk et al (2021) Deconstructing the pharmacological contribution of sphingosine-1 phosphate receptors to mouse models of multiple sclerosis using the species selectivity of ozanimod, a dual modulator of human sphingosine 1-phosphate receptor subtypes 1 and 5. J.Pharmacol.Exp.Ther. 379 379 PMID: 34535564
R Taylor Meadows et al (2018) Ozanimod (RPC1063), a selective S1PR1 and S1PR5 modulator, reduces chronic inflammation and alleviates kidney pathology in murine systemic lupus erythematosus. PLoS One 13 e0193236 PMID: 29608575
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Keywords: Ozanimod, Ozanimod supplier, sphingosine-1-phosphate, receptors, S1P1, S1P5, potent, selective, agonists, agonism, orally, bioavailable, SLE, systemic, lupus, erythematosus, Sphingosine-1-phosphate, Receptors, 7663, Tocris Bioscience
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