货号:A318505
同义名:
奥扎莫德(RPC1063)
/ RPC-1063
Ozanimod是一种口服、每日一次的选择性鞘氨醇 1-磷酸 1 型和 5 型受体调节剂,正在开发用于治疗自身免疫性疾病,包括复发型多发性硬化症(RMS)和溃疡性结肠炎(UC)。
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快速发货 顺丰冷链运输,1-2 天到达
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免费溶解
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]. |
Dose | Mice[1] (p.o.): min = 0.2 mg/kg, max = 3 mg/kg |
Administration | p.o. |
Pharmacokinetics |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.47mL 0.49mL 0.25mL |
12.36mL 2.47mL 1.24mL |
24.72mL 4.94mL 2.47mL |
CAS号 | 1306760-87-1 |
分子式 | C23H24N4O3 |
分子量 | 404.46 |
SMILES Code | N#CC1=CC(C2=NC(C3=CC=CC4=C3CC[C@@H]4NCCO)=NO2)=CC=C1OC(C)C |
MDL No. | MFCD28386168 |
别名 | 奥扎莫德(RPC1063) ;RPC-1063 |
运输 | 蓝冰 |
InChI Key | XRVDGNKRPOAQTN-FQEVSTJZSA-N |
Pubchem ID | 52938427 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, inert atmosphere, room temperature |
溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
|
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 |