product name Ozanimod (RPC1063)
Description: Ozanimod (also known as RPC1063) is a potent and selective oral S1P Receptor 1 modulator. Ozanimod is useful in the treatment of S1P1-associated diseases. The EC50 values of Ozanimod were 160 ± 60 pM and 410 ± 160 pM for S1P1 receptors in the inhibition of cAMP generation and[35S]-GTPγS binding. The 83% Emax value of ozanimod against S1P5 receptor was 11 ± 4.3 nM. RPC1063 dose-dependently decreased S1P1 receptor re-expression on the cell surface and resulted in near complete and sustained loss of cell surface receptor expression at concentrations above 10 nM in S1P1 receptor-HEK293T cells.
References: Br J Pharmacol. 2016 Jun;173(11):1778-92.
404.46
Formula
C23H24N4O3
CAS No.
1306760-87-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 81 mg/mL (200.3 mM)
Water: <1 mg/mL
Ethanol: 10 mg/mL (24.7 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: In S1P1R-HEK293T cells, Ozanimod induces sustained S1P1R internalization and degradation. Kinase Assay: Cell Assay: Ozanimod(RPC1063) was a specific agonist for S1P1 and S1P5 receptors. The EC50values were 160 ± 60 pM and 410 ± 160 pM for S1P1 receptors in the inhibition of cAMP generation and[35S]-GTPγS binding. The 83% Emax value of ozanimod against S1P5 receptor was 11 ± 4.3 nM. RPC1063 dose-dependently decreased S1P1 receptor re-expression on the cell surface and resulted in near complete and sustained loss of cell surface receptor expression at concentrations above 10 nM in S1P1 receptor-HEK293T cells after 1 h incubation. |
|---|---|
| In Vivo | 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. |
| Animal model | MOG-induced EAE model in C57Bl6 mice, TNBS model of inflammatory bowel disease in male Sprague Dawley rats, and Naive CD4+CD45Rbhi T cell adoptive transfer model in SCID mice |
| Formulation & Dosage | Dissolved in 5% DMSO, 5% Tween-20, 90% 0.1N HCl; 0.1-3 mg/kg; oral givage |
| References | Br J Pharmacol. 2016 Jun;173(11):1778-92 |
