Ozanimod
产品说明书
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同义名 : | 奥扎莫德（RPC1063） ;RPC-1063 |
| CAS号 : | 1306760-87-1 | |
| 货号 : | A318505 | |
| 分子式 : | C23H24N4O3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 404.46 | |
| MDL号 : | MFCD28386168 | |
| 存储条件： |
Pure form Keep in dark place, inert atmosphere, room temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 30 mg/mL(74.17 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
IP 2% DMSO+2% Tween80+40% PEG300+water 5 mg/mL clear PO 0.5% CMC-Na 38 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Ozanimod is a specific modulator of S1P1 and S1P5 receptors. It can inhibit the generation of cAMP induced by forskolin, and GTP-binding with EC50 values of 0.16 nM and 0.41 nM, respectively. The induction of S1P1 receptor sustained internalization and degradation could be observed post one-hour treatment with 1 μM Ozanimod in transfected HEK293T cells expressing S1P1 receptors. Oral dose of 1 mg/kg Ozanimod in mice, or 0.5 mg/kg in rat, induced dose-dependent, selective lymphopenia and rapid lymphocyte repopulation kinetics, with reduction of CD4+CCR7+, and CD8+CCR7+ T cells. Administration of 0.6 mg/kg Ozanimod for 14 days reduced ongoing disease symptoms in EAE model induced by immunization with MOG35–55 peptide. Also, a significant reduction of disease activity in TNBS-induced colitis could be achieved in rats dosed 0.3 or 1 mg/kg Ozanimod. Histological disease severity and inflammatory cytokine expression were both reduced in a naïve T-cell adoptive transfer model of colitis after therapeutic administration[1]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.47mL 0.49mL 0.25mL |
12.36mL 2.47mL 1.24mL |
24.72mL 4.94mL 2.47mL |
| 参考文献 |
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