| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C21H20N4O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
RP101075, an active metabolite of Ozanimod, is a potent, orally active agonist of S1PR1 (sphingosine-1-phosphate receptor 1), with an EC50 of 0.27 nM. It shows >100-fold selectivity over S1PR5 (EC50 5.9 nM) and >10000-fold selectivity over S1PR2, S1PR3, and S1PR4, along with a superior cardiovascular safety profile[1]. It is supplied as a white to off-white solid (C21H20N4O2, MW 360.41) at 99.19% purity.
Physical & Chemical Properties
| CAS Number | 1306760-73-5 |
|---|---|
| Molecular Formula | C21H20N4O2 |
| Molecular Weight | 360.41 g/mol |
| Purity | 99.19% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | N#CC1=CC(C2=NC(C3=CC=CC4=C3CC[C@@H]4N)=NO2)=CC=C1OC(C)C |
| Target | S1PR1, S1PR5 |
| Signaling Pathway | GPCR/G Protein; Metabolic Enzyme/Protease |
| Solubility | In Vitro: DMSO: 50 mg/mL (138.73 mM; Requires sonication and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
S1PR1 0.27 nM (EC50) |
S1PR5 5.9 nM (EC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 50 mg/mL (138.73 mM) | requires sonication and warming and heat to 60°C; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 5 mg/mL (13.87 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (50.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vivo
In intracerebral hemorrhage (ICH) mice, RP101075 (0.3-0.6 mg/kg; p.o.) significantly attenuated neurological deficits and reduced brain edema. After ICH, RP101075 lowered cytokine expression and the counts of brain-infiltrating lymphocytes, neutrophils, and microglia. ICH mice treated with RP101075 also showed improved blood-brain barrier integrity and reduced neuronal death[1]. Lymphocytes and pDC in mouse spleens are inhibited by RP101075 (0.3-3 mg/kg; p.o.; daily from week 23 until week 42)[2].
| Animal Model | NZBWF1 female mice[2] |
|---|---|
| Dosage | 0.3, 1, 3 mg/kg |
| Administration | P.o.; daily from week 23 until week 42 |
| Result | Dose-dependent reduction in lymphocytes in the spleen following 20 weeks of treatment; a reduction in plasmacytoid dendritic cells (pDC). |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Need this compound in a format that drops straight into your assay? We can tailor formulation, chemistry, and documentation so your results stay consistent across runs and re-orders.
- Format options: solid or pre-dissolved solution (choose solvent), target concentration, aliquots, light/moisture-protected packaging
- Chemistry options: free base/acid vs salt forms, hydrate/solvate preference, stereoisomer control (single enantiomer or racemate), close analogs
- Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
- QC & documentation: standard COA or enhanced analytical pack (HPLC/LC-MS/NMR), chiral purity, residual solvents, water content (KF), method-specific specs
- Scale & continuity: mg to gram scale, bulk pricing, lot reservation, repeat-order continuity
To quote quickly, tell us: compound name + CAS/structure (SMILES or mol file), intended assay context, solvent preference, salt/stereochemistry requirements, purity/QC level, and the amount (mg–g).
Can’t find the compound you’re looking for?
Send the CAS or structure and your specs. We can help source it, suggest close equivalents, or discuss custom synthesis with the right QC documentation (RUO).
METTL3-mediated ANXA2 inhibition confers neuroprotection in ischemic stroke: Evidence from in vivo and in vitro studies. FASEB J 2023 Jul;37(7):e22974. PMID: 37249328
