Ozanimod 是一种选择性S1P1和S1P5受体激动剂，在[35S]-GTPγS 结合实验中，EC50分别为 410 pM 和 11 nM。它可研究治疗克罗恩病、溃疡性结肠炎、多发性硬化症和复发性多发性硬化症的试验。

Ozanimod (RPC1063) is a specific oral S1P Receptor 1 modulator. Ozanimod has been used in trials studying the treatment of Crohn's Disease, Ulcerative Colitis, Multiple Sclerosis, and Relapsing Multiple Sclerosis.

In S1P1R-HEK293T cells, Ozanimod induces sustained S1P1R internalization and degradation. [1]

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 Clinicalal symptoms. In a rat TNBS model of inflammatory bowel disease, Ozanimod (1.2 mg/kg, p.o.) inhibits Clinicalal and histological disease scores. In a Na?ve 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. [1]

1306760-87-1

C23H24N4O3

404.47

奥扎莫德;RPC-1063

DMSO:75 mg/mL (185.4 mM)
Ethanol:10 mg/mL (24.72 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years