规格

价格

库存

数量

1 mg

¥ 549

现货

2 mg

¥ 685

现货

5 mg

¥ 892

现货

10 mg

¥ 1,380

现货

25 mg

¥ 2,530

现货

50 mg

¥ 3,780

现货

100 mg

¥ 5,450

现货

200 mg

¥ 7,630

现货

1 mL x 10 mM (in DMSO)

¥ 1,090

现货

生物活性

产品描述	Omaveloxolone (RTA-408) is an oral, potent, and selective activator of the nuclear factor erythropoietin-related factor 2 (Nrf2) pathway, as well as a low-potency PPARγ agonist. Omaveloxolone inhibits osteoclast formation by suppressing the STING-dependent NF-κB signaling pathway. Omaveloxolone is being investigated for use in ALS, multiple sclerosis, non-alcoholic steatohepatitis, neurodegenerative diseases, and oncology research.
靶点活性	Human tumor cells:260 nM (GI50), HT29 cells:1.41 μM (EC50), L929 cells:5.25 μM (EC50), NO:4.4 ± 1.8 nM
体外活性	方法：HT22 细胞加入 Omaveloxolone（100， 500， 1000 nM），处理 24 小时，Western blot 检测 NRF2， HO-1， NQO1。结果：Omaveloxolone 剂量依赖性上调 NRF2、HO-1 和 NQO1 蛋白水平。[1] 方法：人 FA 患者皮肤成纤维细胞加入 Omaveloxolone （50 nM）或 DMF （10 μM），处理 48 小时，DCFDA 荧光探针检测活性氧（ROS）水平。结果：Omaveloxolone 显著降低 FA 细胞的基础 ROS 水平。[2]
体内活性	方法：10 月龄 APP/PS1 转基因小鼠(AD 模型)及野生型(WT)对照，腹腔注射 Omaveloxolone (1 mg/kg/天，每日一次)，连续注射 2 个月。结果： Omaveloxolone 显著提高 APP/PS1 小鼠的 Y 迷宫交替率和水迷宫穿越平台次数及目标象限停留时间，改善认知功能。[1] 方法：心脏/骨骼肌特异性 Fxn 基因敲除小鼠(FXN-cKO)，从 3 周龄开始给药，混入花生酱口服方式给予 Omaveloxolone (24 mg/kg/天)，从 3 周龄给药至 8 周龄(共 5 周)。结果：Omaveloxolone 显著改善心功能：EF 从 26%提高到 47.5%(P<0.001)，FS 从 22%提高到 42.5%。[2]
细胞实验	For growth inhibition assays, cells are plated in duplicate 96-well culture dishes at 3 x 103 cells per well. The following day, one plate is treated with RTA 408 and the other is immediately processed for the sulforhodamine B (SRB) assay (time 0). Cells in the RTA 408-treated plate are processed for the SRB assay 72 hours after the start of treatment. Percentage of growth relative to vehicle-treated cells is calculated using: [(Ti-Tz)/(C-Tz)] x 100 where (Tz) is the absorbance value at time zero, (C) is absorbance value from vehicle treated wells after 72 hours, and (Ti) is the absorbance value from wells treated with the drug. Dose-response curves are plotted in GraphPad Prism and GI50 values are calculated(Only for Reference)
别名	RTA-408

化学信息

分子量	554.71
分子式	C₃₃H₄₄F₂N₂O₃
CAS No.	1474034-05-3
Smiles	[H][C@@]12CC(C)(C)CC[C@@]1(CC[C@]1(C)[C@]2([H])C(=O)C=C2[C@@]1(C)CC[C@@]1([H])C(C)(C)C(=O)C(=C[C@]21C)C#N)NC(=O)C(C)(F)F
密度	1.19 g/cm3 (Predicted)

储存&溶解度

存储

Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

实际储存温度请以COA为准

溶解度信息

Ethanol: 16 mg/mL (28.84 mM), Sonication is recommended.

DMSO: 240 mg/mL (432.66 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

体内实验配方

10% DMSO+90% Corn Oil: 3.3 mg/mL (5.95 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.8027 mL	9.0137 mL	18.0274 mL	90.1372 mL
5 mM	0.3605 mL	1.8027 mL	3.6055 mL	18.0274 mL
10 mM	0.1803 mL	0.9014 mL	1.8027 mL	9.0137 mL
20 mM	0.0901 mL	0.4507 mL	0.9014 mL	4.5069 mL

DMSO

	1mg	5mg	10mg	50mg
50 mM	0.0361 mL	0.1803 mL	0.3605 mL	1.8027 mL
100 mM	0.0180 mL	0.0901 mL	0.1803 mL	0.9014 mL

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

Omaveloxolone

Omaveloxolone

产品介绍

引用文献

计算器

体内实验配液计算器

剂量转换

关键词

Omaveloxolone

Omaveloxolone

Omaveloxolone 相关产品

产品介绍

引用文献

计算器

体内实验配液计算器

剂量转换

关键词