GLX351322
目录号 : GC31367
GLX351322是一种NADPH氧化酶4 (NOX4)抑制剂，IC50值为5μM。
Cas No.:835598-94-2
Sample solution is provided at 25 µL, 10mM.
GLX351322 is a NADPH Oxidase 4 (NOX4) inhibitor, with an IC50 value of 5μM [1]. GLX351322 inhibits ROS/MAPK/NF-κB signaling pathways, exhibiting anti-inflammatory effect[2]. GLX351322 has been widely used in various animal models to regulate neural functions and reduce oxidative stress[3].
In vitro, GLX351322 (10μM) treatment for 3 hours reduced the production of reactive oxygen species (ROS) and cell death in human islet cells induced by high glucose and palmitate[4]. Treatment with 40μM GLX351322 for 24 hours inhibited the proliferation of hypoxia-induced leiomyoma cells and promoted cell apoptosis[5]. Treatment with 5μM GLX351322 for 48 hours enhanced the cell death of BCPAP and TPC-1 cells treated with Lenvatinib[6].
In vivo, GLX351322 treatment via oral administration at a dose of 3.8mg/kg/day for 2 weeks suppressed tumor growth and progression in Gl261 glioma cell-intracranial xenograft mice [7]. Continuous intraperitoneal injection of 5mg/kg/day dose of GLX351322 for four consecutive weeks rescued synaptic and memory deficits, and decreased oxidative stress and amyloid levels in the hippocampus of APP/PS1 mice [8].
References:
[1] Anvari E, Wikström P, Walum E, et al. The novel NADPH oxidase 4 inhibitor GLX351322 counteracts glucose intolerance in high-fat diet-treated C57BL/6 mice[J]. Free radical research, 2015, 49(11): 1308-1318.
[2] Zhen J, Chen X, Mao Y, et al. GLX351322, a Novel NADPH Oxidase 4 Inhibitor, Attenuates TMJ Osteoarthritis by Inhibiting the ROS/MAPK/NF‐κB Signaling Pathways[J]. Oxidative Medicine and Cellular Longevity, 2023, 2023(1): 1952348.
[3] Kaur S, Verma R, Sharma V, et al. Targeting NOX inhibitors in neurodegeneration: a therapeutic perspective[J]. Metabolic Brain Disease, 2025, 40(5): 219.
[4] Wang X, Elksnis A, Wikström P, et al. The novel NADPH oxidase 4 selective inhibitor GLX7013114 counteracts human islet cell death in vitro[J]. PLoS One, 2018, 13(9): e0204271.
[5] Miyashita-Ishiwata M, El Sabeh M, Reschke L D, et al. Hypoxia induces proliferation via NOX4-Mediated oxidative stress and TGF-β3 signaling in uterine leiomyoma cells[J]. Free radical research, 2022, 56(2): 163-172.
[6] Tang P, Sheng J, Peng X, et al. Targeting NOX4 disrupts the resistance of papillary thyroid carcinoma to chemotherapeutic drugs and lenvatinib[J]. Cell Death Discovery, 2022, 8(1): 177.
[7] Jiang H, Li F, Cai L, et al. Role of the TSPO–NOX4 axis in angiogenesis in glioblastoma[J]. Frontiers in Pharmacology, 2022, 13: 1001588.
[8] Tao W, Yu L, Shu S, et al. miR-204-3p/Nox4 mediates memory deficits in a mouse model of Alzheimer’s disease[J]. Molecular Therapy, 2021, 29(1): 396-408.
GLX351322是一种NADPH氧化酶4 (NOX4)抑制剂，IC50值为5μM[1]。GLX351322通过抑制ROS/MAPK/NF-κB信号通路发挥抗炎作用[2]。GLX351322已广泛应用于多种动物模型中调节神经功能及减轻氧化应激[3]。
在体外，使用10μM的GLX351322处理人胰岛细胞3小时，可减少高糖和棕榈酸诱导的活性氧(ROS)生成及细胞死亡[4]。用40μM的GLX351322处理平滑肌瘤细胞24小时，能抑制缺氧诱导的细胞增殖并促进凋亡[5]。以5μM的GLX351322处理BCPAP和TPC-1细胞48小时，可增强乐伐替尼诱导的细胞死亡[6]。
在体内，每日口服3.8mg/kg剂量的GLX351322连续2周，能抑制Gl261胶质瘤颅内移植瘤小鼠的肿瘤生长与进展[7]。连续4周每日腹腔注射5mg/kg/day剂量的GLX351322，可挽救APP/PS1小鼠的突触与记忆缺陷，并降低海马区氧化应激水平和淀粉样蛋白沉积[8]。
| Cell experiment [1]: | |
Cell lines | Primary human leiomyoma cells |
Preparation Method | Primary leiomyoma cells were preincubated without serum for 24h. The cells were then incubated in 2% or 21% O2 at 37 C with 10% FBS. After 24h, the media were removed, and the volume of the media was noted. Cells were seeded at a concentration of 0.6×105 cells/ml until 60-70% confluence, and were treated with GLX351322 (40μM) and incubated for 48h. Using 96-well plates, 3000 cells were seeded per well with a complete DMEM/F-12 media. One day after seeding, 20μl of 12μM MTT solution was added to each well, and cells were incubated for 3h. The media was removed, and 100ul/well DMSO was added. The absorbance at 570nm was monitored. |
Reaction Conditions | 40μM; 48h |
Applications | GLX351322 treatment significantly inhibited cell viability of leiomyoma cells exposed to hypoxia. |
| Animal experiment [2]: | |
Animal models | C57Bl/6J mice |
Preparation Method | Six-week-old C57Bl/6J mice were raised in a standard sterile environment. The mouse xenograft models were established by intracranial injection of Gl261 glioma cells (1×106cells/100μl). After the tumors grew for three weeks, all intracranial xenograft mice were divided into two groups: treatment group, which received normal saline (containing 3.8mg/kg of GLX351322) as drinking water daily for two consecutive weeks; control group, which did not receive GLX351322. Each group contained 7 C57Bl/6J mice. The brain tissues of the mice were collected for analysis. |
Dosage form | 3.8mg/kg/day for 2 weeks; p.o. |
Applications | GLX351322 treatment suppressed glioma growth and progression in mice and inhibited angiogenesis. |
References: | |
| Cas No. | 835598-94-2 | SDF | |
| Canonical SMILES | O=C(OCC)C1=C(SC2=C1CCC2)NC(CN3CCN(CC3)C(C4=CC=CO4)=O)=O | ||
| 分子式 | C21H25N3O5S | 分子量 | 431.51 |
| 溶解度 | DMSO : 20 mg/mL (46.35 mM) | 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 | 2.3174 mL | 11.5872 mL | 23.1744 mL |
| 5 mM | 463.5 μL | 2.3174 mL | 4.6349 mL |
| 10 mM | 231.7 μL | 1.1587 mL | 2.3174 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
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Quality Control & SDS
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- Purity: >99.50%
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