Ozanimod

Protein target name:

S1PR1, S1PR5

Mechanism of action:

Agonist

Recommended Concentration for use in cells:

Up to 1 uM

Probe Availability

MedChemExpress

Selleck Chemicals

Probe Information

Target and Probe Information

Target Details

Target class:

GPCR

Subclass:

Sphingosine-1-phosphate receptor

HUGO ID:

HGNC:3165 HGNC:14299

Entrez gene ID:

1901 53637

UNIPROT ID:

P21453 Q9H228

Target alias:

EDG1; S1P1; CD363; ECGF1; EDG-1; CHEDG1; D1S3362; EDG8; S1P5; Edg-8; SPPR-1; SPPR-2

Probe Details

Chemical Probes Portal ID:

CPP2470

Probe alias:

RPC1063, RPC-1063

PubChem CID:

52938427

ChEMBL ID:

CHEMBL3707247

SMILES string:

CC(C)OC1=C(C=C(C=C1)C2=NC(=NO2)C3=C4CC[C@@H](C4=CC=C3)NCCO)C#N

InChi Key:

XRVDGNKRPOAQTN-FQEVSTJZSA-N

Validation in Cells and Model Organisms

In cell validation

On target activity in cells

Potency in cells:

EC50, Emax

0.41 nM, 97% S1PR111 nM, 83% S1PR5

Potency assay (cells):

S1P1R internalization assay

Off target activity in cells

Probe Selectivity in Cell:

Within family: S1PR2 >10000 nM, S1PR3 >10000 nM, S1PR4 7,865 nM

In vivo validation

Organism:

Mouse, Rat

Dose:

0.5 (R), 1 (M) mg/Kg

Route of delivery:

Oral

Systemic clearance:

28 (M), 30 (R) ml/min/Kg

Fraction of probe bound to plasma protein:

4.7 (M), 5.1 (R) h

Cmax:

0.16 (M), 0.06 (R) uM

Tmax:

3 (M), 3 (R) h

Vss:

10 (M), 13 (R) L/Kg

AUC:

1.50 (M), 0.7 (R) uM*h

Primary Reference

Reference (doi):

10.1371/journal.pone.0193236 10.1111/bph.13476

Reference (PMID):

29608575 26990079

Ozanimod

Probe Availability

Probe Information

Target Details

EDG1; S1P1; CD363; ECGF1; EDG-1; CHEDG1; D1S3362; EDG8; S1P5; Edg-8; SPPR-1; SPPR-2

Probe Details

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

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Ozanimod

Probe Availability

Probe Information

Target Details

EDG1; S1P1; CD363; ECGF1; EDG-1; CHEDG1; D1S3362; EDG8; S1P5; Edg-8; SPPR-1; SPPR-2

Probe Details

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?