Ozanimod
Based on 4 publication(s) in Google Scholar
Ozanimod (RPC-1063) is a CNS-penetrant sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod can be used for the research of relapsing multiple sclerosis (MS).
For research use only. We do not sell to patients.
- Purity: 99.98%
- CAS No.: 1306760-87-1
- Formula: C23H24N4O3
- Molecular Weight:404.46
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Ozanimod
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Histological Imaging/Staining
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WB
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Histological Imaging/Staining
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In Vivo Imaging
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Cell Imaging/Staining
Biological Activity
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S1PR1 1.03 nM (EC50) |
S1PR5 8.6 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
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| CHO-K1 | EC50 |
0.16 nM
Compound: RPC1063
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Agonist activity at S1P1 (unknown origin) expressed in CHO-K1 cells using CC4-AM as substrate assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 4 hrs followed by substrate addition and measured after 2 hrs by FRET assay
Agonist activity at S1P1 (unknown origin) expressed in CHO-K1 cells using CC4-AM as substrate assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 4 hrs followed by substrate addition and measured after 2 hrs by FRET assay
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[PMID: 31266686] |
Ozanimod (RPC-1063) has potency and intrinsic activity of S1P receptor modulators for S1P5 across species with [35S]-GTPgS binding, and the EC50 values of 1.03 nM, 1.29 nM, 0.90 nM, 1.02 nM and 0.61 nM for Human S1P1, Cynomolgus monkey S1P1, Mouse S1P1, Rat S1P1 and Canine S1P1, respectively; and the EC50 values of 8.6 nM, 15.9 nM, 957.5 nM, 2032.7 nM and 1662.0 nM for Human S1P5, Cynomolgus monkey S1P5, Mouse S1P5, Rat S1P5 and Canine S1P5, respectively[1].
Ozanimod restores the potency with EC50 from 958 nM for mS1P5 to 6.7 nM for mS1P5_A120T to closely mirror the EC50 for hS1P5 of 8.6 nM by mutating the alanine in the mouse sequence[1].
Ozanimod has binding affinity with Ki values of 2.0 nM, 59.9 nM and 5.6 nM for hS1P5, mS1P5 and mS1P5 _A120T, respectively[1].
Ozanimod has saturation binding of [3H]-ozanimod to hS1P5, and mS1P5_A120T with KD values of 6.56 nM, 7.35 nM, respectively and also has saturation binding for [3H]-A971432 to S1P5D value of 8.75 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ozanimod (oral gavage; 5 mg/kg; once-daily) prevents axonal degradation and myelin loss during toxin challenge but does not facilitate enhanced remyelination after intoxication[1].
Ozanimod (oral, 1 or 5 mg/kg, for 7 days) has good pharmacokinetics in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Experimental Autoimmune Encephalomyelitis Model[1]
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Dosage:0.05, 0.2, or 1 mg/kg
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Administration:oral gavage; 0.05, 0.2, or 1 mg/kg; once daily; for 14 consecutive days
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Result:Attenuated body weight loss, terminal disease scores were significantly attenuated with the 0.2 and 1 mg/kg doses and ALCs were significantly reduced in all dose groups.
Reduced spinal cord inflammation and demyelination, as well as attenuated the number of spinal cord apoptotic cells, and significantly reduced the levels of circulating neurofilament light at the top dose of 1 mg/kg.
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Animal Model:Cuprizone/Rapamycin Demyelination Model[1]
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Dosage:5 mg/kg
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Administration:oral gavage; 5 mg/kg; once-daily
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Result:Protected neuronal axons, preventing breakage and ovoid formation in the corpus callosum of CPZ/Rapa treated mice.
Significantly attenuated the extent to which the corpus callosum demonstrated reduced myelin content as visualized by MRI.
Did not result in enhanced myelin content.
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Animal Model:C57BL/6J mice[1]
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Dosage:1 or 5 mg/kg
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Administration:oral, 1 or 5 mg/kg, for 7 days
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Result:
Dose Terminal body weight % versus day 1 Spinal cord inflammation Foci per 20 cells Spinal cord demyelination Score 0–5 Spinal cord apoptotic cells Count per section Plasma NfL pg/ml Vehicle (5% DMSO, 5%Tween 20, 90% water) 86.4 ± 3.2 8.50 ± 1.21 2.00 ± 0.15 2.25 ± 0.53 4.37 ± 0.89 Ozanimod (0.05 mg/kg) 85.8 ± 2.7 5.00 ± 1.03* 0.91 ± 0.21*** 1.08 ± 0.23* 3.53 ± 0.46 Ozanimod (0.2 mg/kg) 95.7 ± 3.1* 3.54 ± 0.49*** 0.73 ± 0.14 *** 0.91 ± 0.28* 2.62 ± 0.46 Ozanimod (1 mg/kg) 102.8 ± 1.8* 2.67 ± 0.56*** 0.33 ± 0.14 *** 0.60 ± 0.19** 1.91 ± 0.34**
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1306760-87-1
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Appearance Solid
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Molecular Weight 404.46
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Formula C23H24N4O3
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Color White to off-white
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SMILES
N#CC1=CC(C2=NC(C3=CC=CC4=C3CC[C@@H]4NCCO)=NO2)=CC=C1OC(C)C
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Synonyms
RPC-1063
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (4)
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Journal Impact Factor
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Most Recent
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Front Immunol
Selective Sphingosine 1-Phosphate Receptor 1 Modulation Augments Thrombolysis of Low-Dose Tissue Plasminogen Activator Following Cerebrovascular Thrombosis. [Abstract]2022 May 27:13:801727. PMID: 35720286
Ozanimod purchased from MedChemExpress. Usage Cited in: Front Immunol. 2022 May 27:13:801727. [Abstract]
Ketanserin (0.6 mg/kg; 50 µL; i.v.; 90 min) reduced thrombus volume in C57BL/6 mice treated with tPA.
Ozanimod purchased from MedChemExpress. Usage Cited in: Front Immunol. 2022 May 27:13:801727. [Abstract]
Ketanserin (0.6 mg/kg; 50 µL; i.v.; 90 min) reduced the counts of CD3+ T cells and CD45+ cells within thrombus of C57BL/6 mice.
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Bioorg Chem
Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]2024 Jun:147:107412. PMID: 38696845 -
Mol Neurobiol
Ozanimod-Dependent Activation of SIRT3/NF-κB/AIM2 Pathway Attenuates Secondary Injury After Intracerebral Hemorrhage. [Abstract]2023 Mar;60(3):1117-1131. PMID: 36417102
Ozanimod purchased from MedChemExpress. Usage Cited in: Mol Neurobiol. 2023 Mar;60(3):1117-1131. [Abstract]
Ozanimod (0.3-3 mg/kg; i.p.; once daily for 2 d) decreased hematoma size of C57BL/6 mice in the acute phase of ICH.
Ozanimod purchased from MedChemExpress. Usage Cited in: Mol Neurobiol. 2023 Mar;60(3):1117-1131. [Abstract]
Ozanimod (0.3-3 mg/kg; i.p.; once daily for 2 d) downregulated Iba1 and GFAP protein expression in perihematomal brain tissues of C57BL/6 mice after ICH.
Ozanimod purchased from MedChemExpress. Usage Cited in: Mol Neurobiol. 2023 Mar;60(3):1117-1131. [Abstract]
Ozanimod (0.3-3 mg/kg; i.p.; once daily for 2 d) reduced activated glial cells and transitioned microglia from the inflammatory amoeboid state to the ramified state in C57BL/6 mice after ICH.
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bioRxiv
Contribution of S1pr1 -featured astrocyte subpopulation to cisplatin-induced neuropathic pain. [Abstract]2025 Apr 5:2025.04.03.642851. PMID: 40236155
Solvent & Solubility
DMSO : ≥ 29 mg/mL (71.70 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Julie V Selkirk, et al. 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. 2021 Dec;379(3):386-399. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4724 mL | 12.3622 mL | 24.7243 mL | 61.8108 mL |
| 5 mM | 0.4945 mL | 2.4724 mL | 4.9449 mL | 12.3622 mL | |
| 10 mM | 0.2472 mL | 1.2362 mL | 2.4724 mL | 6.1811 mL | |
| 15 mM | 0.1648 mL | 0.8241 mL | 1.6483 mL | 4.1207 mL | |
| 20 mM | 0.1236 mL | 0.6181 mL | 1.2362 mL | 3.0905 mL | |
| 25 mM | 0.0989 mL | 0.4945 mL | 0.9890 mL | 2.4724 mL | |
| 30 mM | 0.0824 mL | 0.4121 mL | 0.8241 mL | 2.0604 mL | |
| 40 mM | 0.0618 mL | 0.3091 mL | 0.6181 mL | 1.5453 mL | |
| 50 mM | 0.0494 mL | 0.2472 mL | 0.4945 mL | 1.2362 mL | |
| 60 mM | 0.0412 mL | 0.2060 mL | 0.4121 mL | 1.0302 mL |
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