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Polmacoxib (CG100649) is a first-in-class, orally active non-steroidal anti-inflammatory compound (NSAID) that acts as a dual inhibitor. It inhibited COX-2 (IC50 ~ 0.1 μg/ml) and carbonic anhydrase. CG100649's interaction with CA in red blood cells provides a new "tissue-specific" transport mechanism designed to deliver sustained levels of the compound to inflamed tissues while maintaining low systemic exposure. Its unique dual COX-2 and CA-binding properties are designed to provide potentially higher safety for cardiovascular, renal and gastrointestinal tissues than conventional NSaids or COX-2 inhibitor drugs. In mouse models, CG100649 inhibited precancerous and malignant colorectal lesions, in part by inhibiting tumor cell proliferation.
| Molecular Weight | 361.39 |
| Formula | C18H16FNO4S |
| CAS Number | 301692-76-2 |
| Solubility (25°C) | DMSO ≥ 200 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related COX Products |
|---|
| Firocoxib
Firocoxib is a selective COX-2 inhibitor exhibiting high selectivity to inhibit COX-2. |
| Celecoxib
Celecoxib is a selective cyclooxygenase-2 (COX-2) inhibitor (IC50 values are 15 and 0.04 μM for COX-1 and COX-2 respectively). |
| Nepafenac
Nepafenac is an analgesic selective inhibitor of COX-2. |
| Ampiroxicam
Ampiroxicam is a nonselective cyclooxygenase inhibitor uesd as anti-inflammatory compound. |
| Bromfenac Sodium
Bromfenac is a nonsteroidal anti-inflammatory compound (NSAID), which has anti-inflammatory activity and may block prostaglandin synthesis by inhibiting cyclooxygenase 1 and 2. |
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