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 |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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