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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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O413886-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $117.90 | |
O413886-10mg | 10mg | In stock | $177.90 | |
O413886-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $365.90 | |
O413886-50mg | 50mg | In stock | $573.90 | |
O413886-100mg | 100mg | In stock | $840.90 |
S1P Receptor Modulators
Synonyms | HY-12288 | 5-[3-[(1~{S})-1-(2-hydroxyethylamino)-2,3-dihydro-1~{H}-inden-4-yl]-1,2,4-oxadiazol-5-yl]-2-propan-2-yloxy-benzenecarbonitrile | D10968 | DTXSID501026488 | Ozanimod [USAN:INN] | RPC1063:RPC-1063 | DB12612 | L04AA38 | AMY3373 | EX-A1316 | 5-{3-[ |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Ozanimod (RPC1063) is a selective oral S1P Receptor 1 modulator. Phase 3. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | AGONIST |
Mechanism of action | Agonist of S1P 1 receptor;Agonist of S1P 2 receptor;Agonist of S1P 3 receptor;Agonist of S1P 4 receptor;Agonist of S1P 5 receptor |
Product Description | Information Ozanimod (RPC1063) Ozanimod (RPC1063) is a selective oral S1P Receptor 1 modulator. Phase 3. Targets S1P1R (Cell-free assay); S1P5R (Cell-free assay) 0.41 nM(EC50); 11 nM(EC50) In vitro In S1P1R-HEK293T cells, Ozanimod induces sustained S1P1R internalization and degradation. 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. |
ALogP | 3.291 |
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HBD Count | 2 |
Rotatable Bond | 7 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC 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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INCHI | 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 |
InChi Key | XRVDGNKRPOAQTN-FQEVSTJZSA-N |
Canonical SMILES | CC(C)OC1=C(C=C(C=C1)C2=NC(=NO2)C3=C4CCC(C4=CC=C3)NCCO)C#N |
Isomeric SMILES | CC(C)OC1=C(C=C(C=C1)C2=NC(=NO2)C3=C4CC[C@@H](C4=CC=C3)NCCO)C#N |
PubChem CID | 52938427 |
Molecular Weight | 404.46 |
PubChem CID | 52938427 |
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CAS Registry No. | 1306760-87-1 |
DrugCentral Ligand | 5383 |
RCSB PDB Ligand | JEU |
GPCRdb Ligand | ozanimod |
Enter Lot Number to search for COA:
Solubility | Solubility (25°C) In vitro DMSO: 81 mg/mL (200.26 mM); Ethanol: 10 mg/mL (24.72 mM); Water: Insoluble; |
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DMSO(mg / mL) Max Solubility | 81 |
DMSO(mM) Max Solubility | 200.2670227 |
Water(mg / mL) Max Solubility | <1 |
Pictogram(s) | GHS08, GHS07 |
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Signal | Danger |
Hazard Statements | H302:Harmful if swallowed H372:Causes damage to organs through prolonged or repeated exposure |
Precautionary Statements | P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P260:Do not breathe dust/fume/gas/mist/vapors/spray. P270:Do not eat, drink or smoke when using this product. P319:Get medical help if you feel unwell. |
1. Scott FL, Clemons B, Brooks J, Brahmachary E, Powell R, Dedman H, Desale HG, Timony GA, Martinborough E, Rosen H et al.. (2016) Ozanimod (RPC1063) is a potent sphingosine-1-phosphate receptor-1 (S1P1 ) and receptor-5 (S1P5 ) agonist with autoimmune disease-modifying activity.. Br J Pharmacol, 173 (11): (1778-92). [PMID:26990079] [10.1021/op500134e] |
2. Taylor Meadows KR, Steinberg MW, Clemons B, Stokes ME, Opiteck GJ, Peach R, Scott FL. (2018) Ozanimod (RPC1063), a selective S1PR1 and S1PR5 modulator, reduces chronic inflammation and alleviates kidney pathology in murine systemic lupus erythematosus.. PLoS ONE, 13 (4): (e0193236). [PMID:29608575] [10.1021/op500134e] |
3. Derfuss T, Mehling M, Papadopoulou A, Bar-Or A, Cohen JA, Kappos L. (2020) Advances in oral immunomodulating therapies in relapsing multiple sclerosis.. Lancet Neurol, 19 (4): (336-347). [PMID:32059809] [10.1021/op500134e] |
4. Argollo M, Furfaro F, Gilardi D, Roda G, Allocca M, Peyrin-Biroulet L, Danese S. (2020) Modulation of sphingosine-1-phosphate in ulcerative colitis.. Expert Opin Biol Ther, 20 (4): (413-420). [PMID:32093531] [10.1021/op500134e] |