N-acetyl-2-carboxy Benzenesulfonamide
目录号 : GC16440
A COX-1/COX-2 inhibitor
Cas No.:849067-18-1
Sample solution is provided at 25 µL, 10mM.
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IC50: 0.06 and 0.25 μM for COX-1 and COX-2, respectively
N-acetyl-2-carboxy Benzenesulfonamide is a non-selective inhibitor of COX.
Pharmaceutical inhibition of COX is able to provide relief from the symptoms of inflammation and pain. Nonsteroidal anti-inflammatory drugs, such as aspirin, exert its effect via inhibition of COX.
In vitro: Previous in-vitro COX-1/COX-2 inhibition studies showed that N-acetyl-2-carboxy benzenesulfonamide was a more potent inhibitor than aspirin, and like aspirin. Moreover, N-acetyl-2-carboxy benzenesulfonamide was found to be a nonselective COX-2 inhibitor. In addition, the molecular modeling (docking) study demonstrated that the SO2NHCOCH3 substituent present in N-acetyl-2-carboxy benzenesulfonamide, like the acetoxy substituent in aspirin, was suitably positioned to acetylate the Ser530 hydroxyl group in the COX-2 primary binding site [1].
In vivo: Animal study showed that N-acetyl-2-carboxy benzenesulfonamide and its C-4 2,4-difluorophenyl derivative had superior antiinflammatory activity (oral dosing) in a carrageenan-induced rat paw edema assay compared to aspirin. In addition, N-acetyl-2-carboxy benzenesulfonamide and its C-4 2,4-difluorophenyl derivative exhibited comparable analgesic activity to iflunisal, and superior analgesic activity compared to aspirin [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Chen, Q. H.,Rao, P.N.P., and Knaus, E.E. Design, synthesis, and biological evaluation of N-acetyl-2-carboxybenzenesulfonamides: A novel class of cyclooxygenase-2 (COX-2) inhibitors. Bioorganic & Medicinal Chemistry 13, 2459-2468 (2005).
| Cas No. | 849067-18-1 | SDF | |
| 化学名 | 2-[(acetylamino)sulfonyl]-benzoic acid | ||
| Canonical SMILES | CC(=O)NS(=O)(=O)c1ccccc1C(=O)O | ||
| 分子式 | C9H9NO5S | 分子量 | 243.2 |
| 溶解度 | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | 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 | 4.1118 mL | 20.5592 mL | 41.1184 mL |
| 5 mM | 0.8224 mL | 4.1118 mL | 8.2237 mL |
| 10 mM | 0.4112 mL | 2.0559 mL | 4.1118 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet