CAS NO: | 849067-18-1 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 243.2 |
Cas No. | 849067-18-1 |
Formula | C9H9NO5S |
Solubility | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide |
Chemical Name | 2-[(acetylamino)sulfonyl]-benzoic acid |
Canonical SMILES | CC(=O)NS(=O)(=O)c1ccccc1C(=O)O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
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).