Ketoprofen (Actron) is a non-selective NSAID exhibiting IC50 of 0.5 μM and 2.33 μM for human recombinant COX-1 and COX-2, respectively. It is used for its antipyretic, analgesic, and anti-inflammatory properties by inhibiting cyclooxygenase-1 and -2 (COX-1 and COX-2) enzymes reversibly, which decreases production of pro-inflammatory prostaglandin precursors. Based on in vitro IC (50) COX-1:IC (50) COX-2 ratios, robenacoxib was COX-2 selective (ratio=32.2), diclofenac (ratio=3.9) and meloxicam (ratio=2.7) were only weakly COX-2 preferential, and ketoprofen (ratio=0.049) was COX-1 selective.
Molecular Weight | 254.28 |
Formula | C16H14O3 |
CAS Number | 22071-15-4 |
Solubility (25°C) | DMSO 46 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.
[2] Tiffany Yvonne Loh, et al. Ketoprofen-induced photoallergic dermatitis
[3] Carmen Cantisani, et al. Ketoprofen allergic reactions
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