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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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Purity: ≥98%
Ozanimod (formerly RPC-1063; trade name Zeposia) is a selective and orally bioavailable S1P Receptor 1 modulator that has been approved as an immunomodulatory medication for the treatment of relapsing multiple sclerosis and ulcerative colitis. Ozanimod inhibits the generation of cAMP and[35S]-GTPγS binding by acting as a sphingosine-1-phosphate receptor agonist, with EC50 values of 160 ± 60 pM and 410 ± 160 pM for S1P1 receptors.
| Targets |
S1PR1 ( EC50 = 1.03 nM ); S1PR5 ( EC50 = 8.6 nM )
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
The cAMP (S1P1R) or β-arrestin (S1P4R) signaling was detected by cell signaling assays using the LiveBLAzer-FRET B/G assay. As directed by the manufacturer, assays are carried out in triplicate in 384-well plates. Twenty percent (2-hydoxypropyl)-β-cyclodextrin is used to dilute compound stocks 1:10 at first, and they are kept at 10 mM in 100% DMSO at -50°C. For every 40 times the final assay concentration in 10 mM, a 10-point dose response curve is generated. Hepes 7.4 pH with 0.1% Pluronic F-127. 80 μM forskolin is added to the diluent for the S1P1R assay. To put it briefly, 104 cells per well are cultured for 4 hours at 37°C with a dose response of ligand available. Probenecid and CC4-AM substrate are added, and after an additional two hours of incubation at 37°C, the sample is examined using a Spectramax M5. Data for S1P1R cAMP assays is normalized to the highest fluorescence produced by 2 μM forskolin. In GTPγS binding assays, 1–5 μg/well of membrane protein is incubated for 15 minutes in 96-well plates 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. The plates are incubated for 120 minutes after the addition of compound and 200 pM GTP [35S] 1250Ci/mmol, and then centrifuged for 5 minutes at 300g. A TopCount Instrument is used to detect radioactivity. A four-parameter variable called slope is used to fit all of the data. Radioactivity is detected with a TopCount Instrument. GraphPad Prism's four parameter variable slope non-linear regression is used to fit all the data in order to determine the maximum efficacy and half-maximum effective concentration (EC50) in relation to S1P.
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| Cell Assay |
Ozanimod (RPC1063) was a particular agonist for S1P1 and S1P5 receptors. The suppression of cAMP generation and [35S]-GTPγS binding by S1P1 receptors had EC50 values of 160 ± 60 pM and 410 ± 160 pM, respectively. In relation to the S1P5 receptor, ozanimod's 83% Emax value was 11 ± 4.3 nM. After one hour of incubation, RPC1063 virtually completely and persistently reduced S1P1 receptor re-expression on the cell surface in S1P1 receptor-HEK293T cells. This was observed at concentrations greater than 10 nM.
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| References |
| Molecular Formula |
C23H24N4O3
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| Molecular Weight |
404.46
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| Exact Mass |
404.18
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| Elemental Analysis |
C, 68.30; H, 5.98; N, 13.85; O, 11.87
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| CAS # |
1306760-87-1
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| Related CAS # |
Ozanimod hydrochloride; 1618636-37-5
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| Appearance |
Solid powder
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| SMILES |
CC(C)OC1=C(C=C(C=C1)C2=NC(=NO2)C3=C4CC[C@@H](C4=CC=C3)NCCO)C#N
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| InChi Key |
XRVDGNKRPOAQTN-FQEVSTJZSA-N
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| 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
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| Chemical Name |
5-[3-[(1S)-1-(2-hydroxyethylamino)-2,3-dihydro-1H-inden-4-yl]-1,2,4-oxadiazol-5-yl]-2-propan-2-yloxybenzonitrile
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 5%DMSO + Corn oil: 2.0mg/ml (4.94mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4724 mL | 12.3622 mL | 24.7243 mL | |
| 5 mM | 0.4945 mL | 2.4724 mL | 4.9449 mL | |
| 10 mM | 0.2472 mL | 1.2362 mL | 2.4724 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02531126 | Active Recruiting |
Drug: RPC1063 | Ulcerative Colitis | Celgene | December 2, 2015 | Phase 3 |
| NCT03915769 | Active Recruiting |
Drug: Ozanimod Other: Placebo |
Colitis, Ulcerative | Celgene | June 3, 2019 | Phase 3 |
| NCT04140305 | Active Recruiting |
Drug: RPC-1063 | Multiple Sclerosis | Celgene | January 16, 2020 | Phase 3 |
| NCT06133049 | Active Recruiting |
Drug: Ozanimod Drug: No DMTs |
Multiple Sclerosis | Bristol-Myers Squibb | March 16, 2021 | N/A |
| NCT05605782 | Active Recruiting |
N/A | Multiple Sclerosis, Relapsing -Remitting |
Bristol-Myers Squibb | June 30, 2022 | N/A |
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