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Ozanimod (RPC1063) - 98%, high purity , CAS No.1306760-87-1, 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

  • Moligand™
  • ≥98%
Item Number
O413886
Grouped product items
SKUSizeAvailabilityPrice Qty
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

Basic Description

SynonymsOzanimod|1306760-87-1|RPC1063|RPC-1063|Ozanimod (RPC1063)|(S)-5-(3-(1-((2-hydroxyethyl)amino)-2,3-dihydro-1H-inden-4-yl)-1,2,4-oxadiazol-5-yl)-2-isopropoxybenzonitrile|Z80293URPV|RPC 1063|UNII-Z80293URPV|Benzonitrile, 5-(3-((1S)-2,3-dihydro-1-((2-hydroxye
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsOzanimod (RPC1063) is a selective oral S1P Receptor 1 modulator. Phase 3.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeAGONIST
Mechanism of actionAgonist 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.

Product Properties

ALogP3.291
HBD Count2
Rotatable Bond7

Associated Targets

CX3CR1 Tchem CX3C chemokine receptor 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GPR35 Tchem G-protein coupled receptor 35 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRD4 Tchem Bromodomain-containing protein 4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

S1PR5 Tclin Sphingosine 1-phosphate receptor 5 5 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

S1PR2 Tchem Sphingosine 1-phosphate receptor 2 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

S1PR4 Tclin Sphingosine 1-phosphate receptor 4 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FFAR4 Tchem Free fatty acid receptor 4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FPR2 Tchem N-formyl peptide receptor 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CSNK1D Tchem Casein kinase I isoform delta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

S1PR1 Tclin Sphingosine 1-phosphate receptor 1 7 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

S1PR3 Tclin Sphingosine 1-phosphate receptor 3 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRIM24 Tchem Transcription intermediary factor 1-alpha 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

C5AR1 Tclin C5a anaphylatoxin chemotactic receptor 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRPF1 Tchem Peregrin 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKA Tchem Aurora kinase A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADRB2 Tclin Beta-2 adrenergic receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

APLNR Tchem Apelin receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADRA2A Tclin Alpha-2A adrenergic receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADGRF1 Tbio Adhesion G-protein coupled receptor F1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AGTR1 Tclin Type-1 angiotensin II receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GPR119 Tclin Glucose-dependent insulinotropic receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GLP1R Tclin Glucagon-like peptide 1 receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAPK1 Tchem Mitogen-activated protein kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

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
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

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section

3 results found

Lot NumberCertificate TypeDateItem
I2208115Certificate of AnalysisJul 06, 2022 O413886
I2208116Certificate of AnalysisJul 06, 2022 O413886
I2208117Certificate of AnalysisJul 06, 2022 O413886

Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 81 mg/mL (200.26 mM); Ethanol: 10 mg/mL (24.72 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility81
DMSO(mM) Max Solubility200.2670227
Water(mg / mL) Max Solubility<1

Safety and Hazards(GHS)

Pictogram(s) GHS08,   GHS07
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.

Related Documents

References

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]
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]
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]
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]

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