|N-acetyl-2-carboxy Benzenesulfonamide Catalog No.GC16440|
Sample solution is provided at 25 µL, 10mM.
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|Chemical Name||2-[(acetylamino)sulfonyl]-benzoic acid|
|Solubility||≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide||Storage||Store at -20°C|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
|Shipping Condition||Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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 .
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 .
Clinical trial: So far, no clinical study has been conducted.
 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).