Omaveloxolone (RTA-408)
(Synonyms: RTA 408) 目录号 : GC13693
Omaveloxolone (RTA-408)是一种抗氧化炎症调节剂（AIM），可激活Nrf2并抑制一氧化氮（NO）的生成。
Cas No.:1474034-05-3
Sample solution is provided at 25 µL, 10mM.
Omaveloxolone (RTA-408) is an antioxidant inflammation modulator (AIM), which activates Nrf2 and suppresses nitric oxide (NO)[1]. Omaveloxolone is usually used in research related to inflammation, oxidative stress and Friedreich Ataxia [2][3].
In vitro, Omaveloxolone (0.15-4.8μM; 24h) induced ferroptosis in cisplatin-resistant A549/DDP lung adenocarcinoma cells, downregulated WWP1, stabilized NCOA4, promoted ferritinophagy, and triggered iron overload, lipid peroxidation, and cell death[4]. Omaveloxolone (0-500nM; 72h) reduced cell viability in EB-associated SCC cell lines and normal human epidermal keratinocytes in a dose-dependent manner[5].
In vivo, Omaveloxolone (17.5mg/kg/day; i.p.; 3 days) significantly increased 35-day survival and restored normal hematopoietic stem and progenitor cell frequency and function in C57BL/6 mice exposed to 7.5 Gy total body irradiation[6]. Omaveloxolone (100μg/kg; i.p.; 24h before surgery) significantly reduced serum creatinine and blood urea nitrogen levels, decreased renal tubular necrosis and ROS production, and enhanced Nrf2 nuclear translocation and GSH-related antioxidant gene expression in Nrf2-deficient male C57BL/6J mice subjected to unilateral renal ischemia-reperfusion injury[7].
References:
[1] Probst BL, Trevino I, McCauley L, et al. RTA 408, A Novel Synthetic Triterpenoid with Broad Anticancer and Anti-Inflammatory Activity. PLoS One. 2015;10(4):e0122942.
[2] Hao J, Zhou J, Hu S, et al. RTA 408 ameliorates diabetic cardiomyopathy by activating Nrf2 to regulate mitochondrial fission and fusion and inhibiting NF-κB-mediated inflammation. Am J Physiol Cell Physiol. 2024;326(2):C331-C347.
[3] Lee A. Omaveloxolone: First Approval. Drugs. 2023;83(8):725-729.
[4] Wang X, Liu T, Fei Y, et al. RTA-408 overcomes cisplatin-resistant lung cancer by inhibiting WWP1-mediated NCOA4 ubiquitination to induce ferritinophagy and ferroptosis. Free Radic Biol Med. 2025;238:595-610.
[5] Cohen-Nowak AJ, Cohen AJ, Correia ED, Portocarrero CP, South AP, Nikbakht N. Omaveloxolone attenuates squamous cell carcinoma growth and disease severity in an Epidermolysis Bullosa mouse model. Exp Dermatol. 2022;31(7):1083-1088.
[6] Goldman DC, Alexeev V, Lash E, Guha C, Rodeck U, Fleming WH. The triterpenoid RTA 408 is a robust mitigator of hematopoietic acute radiation syndrome in mice. Radiat Res. 2015;183(3):338-344.
[7] Han P, Qin Z, Tang J, et al. RTA-408 Protects Kidney from Ischemia-Reperfusion Injury in Mice via Activating Nrf2 and Downstream GSH Biosynthesis Gene. Oxid Med Cell Longev. 2017;2017:7612182.
Omaveloxolone (RTA-408)是一种抗氧化炎症调节剂（AIM），可激活Nrf2并抑制一氧化氮（NO）的生成[1]。Omaveloxolone常用于炎症、氧化应激以及弗里德赖希共济失调相关的研究[2][3]。
体外实验中，Omaveloxolone（0.15-4.8μM；24小时）可在顺铂耐药的A549/DDP肺腺癌细胞中诱导铁死亡，表现为下调WWP1、稳定NCOA4、促进铁蛋白自噬，并引发铁过载、脂质过氧化和细胞死亡[4]。Omaveloxolone（0-500nM；72小时）还可剂量依赖性地降低EB相关鳞状细胞癌细胞及正常人表皮角质形成细胞的活力[5]。
体内实验中，Omaveloxolone（17.5mg/kg/天；腹腔注射；连续3天）显著提高了接受7.5 Gy全身照射的C57BL/6小鼠35天存活率，并恢复了其正常的造血干/祖细胞频率与功能[6]。Omaveloxolone（100μg/kg；腹腔注射；手术前24小时）显著降低了单侧肾缺血再灌注损伤Nrf2缺失雄性C57BL/6J小鼠的血清肌酐和尿素氮水平，减少肾小管坏死和ROS生成，并增强了Nrf2核转位及GSH相关抗氧化基因的表达[7]。
| Cell experiment [1]: | |
Cell lines | Human colorectal adenocarcinoma cell lines HT-29 and HCT-116 |
Preparation Method | A549/DDP cell line was cultured in RPMI-1640 medium supplemented with 10% fetal bovine serum from the same supplier, along with 5mg/mL of penicillin/streptomycin. To preserve their resistance to Cisplatin (DDP), A549/DDP cells were routinely exposed to 1μg/mL of DDP. Cells in the logarithmic growth phase were collected and treated with trypsin to generate a uniform single-cell suspension. The cells were then seeded into six-well plates at a density of 500 cells per 10μL of culture medium. Following seeding, the cells were treated with a range of Omaveloxolone concentrations-0, 0.15, 0.3, 0.6, 1.2, 2.4, and 4.8μM for 24h to evaluate the compound’s effects on cell viability and proliferation. Cellular ferrous iron content was determined using a commercial iron detection kit. Protein was ectracted for Western blotting analysis. |
Reaction Conditions | 0.15-4.8μM; 24h |
Applications | Omaveloxolone induced ferroptosis in cisplatin-resistant A549/DDP lung adenocarcinoma cells, downregulated WWP1, stabilized NCOA4, promoted ferritinophagy, and triggered iron overload and cell death. |
| Animal experiment [2]: | |
Animal models | Nrf2-deficient male C57BL/6J mice |
Preparation Method | 24h before surgery, Nrf2-deficient male C57BL/6J mice were intraperitoneally administered with Omaveloxolone (100μg/kg body weight) or 0.1% DMSO in PBS as the vehicle. A unilateral ischemia with simultaneous contralateral nephrectomy mouse model was made by surgery. The blood samples were obtained from the inferior vena cava at a designated timing point after reperfusion. The blood urea nitrogen and serum creatinine levels were measured by commercially available assay kits to assess renal function. The left kidney tissues harvested at 24h postischemia were fixed for Kidney Histology and Immunohistochemistry analyses. Malondialdehyde (MDA), carbonylated protein, total antioxidant capacity (T-AOC), total glutathione (T-GSH), and glutathione to glutathione disulfide (GSH/GSSG) ratio in the supernatant of renal cortical homogenate were estimated by using each assay kit, according to the manufacturer’s instructions. |
Dosage form | 100μg/kg; i.p.; 24h before surgery |
Applications | Omaveloxolone (100μg/kg; i.p.; 24h before surgery) significantly reduced serum creatinine and blood urea nitrogen levels, decreased renal tubular necrosis, and enhanced Nrf2 nuclear translocation and GSH-related antioxidant gene expression in Nrf2-deficient male C57BL/6J mice subjected to unilateral renal ischemia-reperfusion injury. |
References: | |
| Cas No. | 1474034-05-3 | SDF | |
| 别名 | RTA 408 | ||
| 分子式 | C33H44F2N2O3 | 分子量 | 554.71 |
| 溶解度 | ≥ 55.5mg/mL in DMSO, ≥ 25.05mg/mL in EtOH | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8027 mL | 9.0137 mL | 18.0274 mL |
| 5 mM | 360.5 μL | 1.8027 mL | 3.6055 mL |
| 10 mM | 180.3 μL | 901.4 μL | 1.8027 mL |
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动物平均体重 | g | |
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动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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2.
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