Polmacoxib (CG100649) 是一流的口服活性非甾体抗炎药 (NSAID)，它是 COX-2（IC50 约为 0.1 μg/ml）和碳酸酐酶的双重抑制剂。 Polmacoxib 在小鼠模型中抑制结直肠腺瘤和肿瘤生长。
| Cas No. | 301692-76-2 |
| 别名 | 帕马考昔,CG100649 |
| 化学名 | 4-[3-(3-fluorophenyl)-4,5-dihydro-5,5-dimethyl-4-oxo-2-furanyl]-benzenesulfonamide |
| Canonical SMILES | FC1=CC(C2=C(C3=CC=C(S(N)(=O)=O)C=C3)OC(C)(C)C2=O)=CC=C1 |
| 分子式 | C18H16FNO4S |
| 分子量 | 361.4 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2)(1:8): 0.5 mg/ml,Ethanol: 5 mg/ml |
| 储存条件 | 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. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Polmacoxib is an inhibitor of cyclooxygenase 2 (COX-2) and the carbonic anhydrase subtypes I (CAI) and CAII. It inhibits COX-2 in the absence of carbonic anhydrase II with an IC50 value of 40 nM, which increases by approximately 4- and 17-fold in the presence of a CAII at a molar ratio of 1:1 and 1:5, respectively. It also inhibits CAI and CAII (IC50s = 210 and 95 nM, respectively). Polmacoxib prevents >95 and 90% of prostaglandin E2 (PGE2) production in HCA-7 and HT-29 human colon cancer cells, respectively, using concentrations of 0.01 and 0.001 ug/ml. It inhibits polyp formation in a transgenic mouse model of intestinal polyp formation and tumor growth in human colorectal carcinoma mouse xenograft models when used at a dose of 7 mg/kg. The inhibition of COX-2 and CAII by polmacoxib has the potential for fewer serious systemic adverse effects, including cardiovascular events associated with COX-2 selective inhibitors such as celecoxib . Formulations containing polmacoxib have been used in the treatment of osteoarthritis. |
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