Ozanimod (CAS 1306760-87-1), also known as RPC1063, is a selective, orally bioavailable sphingosine 1-phosphate receptor 1 (S1P₁) modulator . Structurally, Ozanimod features a complex molecular architecture centered on a 1,2,4-oxadiazole core linking an indane-amine moiety to a cyanophenyl isopropoxy group, with a molecular formula of C₂₃H₂₄N₄O₃ and a molecular weight of 404.46 g/mol . The molecule contains a chiral center at the indane 1-position, with the (S)-enantiomer being the active pharmacological form .
Ozanimod is a clinically approved, once-daily oral sphingosine 1-phosphate receptor modulator for the treatment of relapsing multiple sclerosis (MS) and inflammatory bowel disease . As a selective S1P₁ modulator, Ozanimod induces sustained internalization and degradation of S1P₁ receptors, preventing lymphocyte egress from lymph nodes and reducing the number of circulating lymphocytes available to mediate autoimmune inflammation . Ozanimod was developed by Celgene (now Bristol-Myers Squibb) and received FDA approval on March 26, 2020, followed by approval in Canada in October 2020 and European Commission approval for relapsing remitting multiple sclerosis in November 2021 . In pharmaceutical quality control contexts, Ozanimod and its related substances serve as essential reference standards for analytical method development, impurity profiling, and regulatory filings. The unique structural features of Ozanimod—particularly the chiral indane-amine moiety and the 1,2,4-oxadiazole linker—provide a rigid, conformationally constrained scaffold that facilitates high-affinity binding to S1P₁, making this compound a valuable tool in immunology drug discovery and a benchmark for developing next-generation S1P receptor modulators.
Product Parameters
Parameter
Specification
Product Name
Ozanimod
CAS Number
1306760-87-1
Molecular Formula
C₂₃H₂₄N₄O₃
Molecular Weight
404.46 g/mol
Appearance
Solid powder
Melting point
134-137 °C
Boiling Point
648.3±65.0 °C
Density
1.30±0.1 g/cm3(Predicted)
Storage Condition
Powder: –20°C for 3 years; in solvent: –20°C for 6 months
Application
Ozanimod is primarily indicated for the treatment of multiple sclerosis, ulcerative colitis, and Crohn's disease. Among these conditions, multiple sclerosis and ulcerative colitis are characterized not only by a prolonged disease course and high incidence rates but also by the requirement for long-term medication. It is evident that ozanimod has a substantial market potential and promising future prospects.
Bioactivity
Ozanimod (RPC1063) is a selective oral S1P Receptor 1 modulator. Phase 3 clinical trial.
In Vivo Studies
In vitro, ozanimod demonstrates high oral bioavailability and a large volume of distribution. In an MOG-induced EAE mouse model, ozanimod (3 mg/kg, p.o.) inhibited clinical symptoms. In a TNBS-induced rat model of inflammatory bowel disease, ozanimod (1.2 mg/kg, p.o.) suppressed both clinical and histological disease progression. In a natural CD4+CD45Rbhi T-cell adoptive transfer model, ozanimod (1.2 mg/kg, p.o.) also significantly reduced disease severity, as assessed by measurements of inflammation, glandular loss, hyperplasia, neutrophil infiltration, and mucosal thickness.
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