3,4-Dihydroquinolin-2(1H)-one
(Synonyms: 3,4-二氢-2(1H)-喹啉酮) 目录号 : GC46557
A building block
Cas No.:553-03-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
3,4-Dihydroquinolin-2(1H)-one is a building block.1,2 It has been used in the synthesis of compounds with antidepressant and anticonvulsant activities, as well as dual ligands of sigma (σ) receptors and the NMDA receptor GluN2b subunit that have antioxidant and neuroprotective properties.
1.Deng, X.-Q., Song, M.-X., Zheng, Y., et al.Design, synthesis and evaluation of the antidepressant and anticonvulsant activities of triazole-containing quinolinonesEur. J. Med. Chem.73217-224(2014) 2.Zampieri, D., Fortuna, S., Calabretti, A., et al.Discovery of new potent dual sigma receptor/GluN2b ligands with antioxidant property as neuroprotective agentsEur. J. Med. Chem.180268-282(2019)
| Cas No. | 553-03-7 | SDF | |
| 别名 | 3,4-二氢-2(1H)-喹啉酮 | ||
| Canonical SMILES | O=C1NC2=C(CC1)C=CC=C2 | ||
| 分子式 | C9H9NO | 分子量 | 147.2 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml | 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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 6.7935 mL | 33.9674 mL | 67.9348 mL |
| 5 mM | 1.3587 mL | 6.7935 mL | 13.587 mL |
| 10 mM | 0.6793 mL | 3.3967 mL | 6.7935 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.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Novel 3,4-Dihydroquinolin-2(1H)-one derivatives as dual inhibitor targeting AKR1B1/ROS for treatment of diabetic complications: Design, synthesis and biological evaluation
Bioorg Chem 2020 Dec;105:104428.PMID:33161249DOI:10.1016/j.bioorg.2020.104428.
AKR1B1 (Aldose reductase) has been used as therapeutic intervention target for treatment of diabetic complications over 50 years, and more recently for inflammation and cancer. However, most developed small molecule inhibitors have the defect of low bioactivity. To address this limitation, novel series of 3,4-Dihydroquinolin-2(1H)-one derivatives as dual inhibitor targeting AKR1B1/ROS (Reactive Oxygen Species) were designed and synthesized. Most of these derivatives were found to be potent and selective against AKR1B1, and compound 8a was the most active with an IC50 value of 0.035 μM. Moreover, some prepared derivatives showed strong anti-ROS activity, and among them the phenolic 3,5-dihydroxyl compound 8b was proved to be the most potent, even comparable to that of the well-known antioxidant Trolox at a concentration of 100 μM. Thus the results suggested a success in the construction of potent dual inhibitor for the therapeutic intervention target of AKR1B1/ROS.