For research use only.
CAS No. 53716-49-7
Carprofen inhibits canine COX2 with IC50 of 30 nM.
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|Description||Carprofen inhibits canine COX2 with IC50 of 30 nM.|
|Features||Potency of carprofen for canine COX2 is more than 100-fold greater relative to canine COX1.|
Carprofen (S and R stereoisomers) inhibits canine COX2 with IC50 of 0.102 microM for the racemic mixture, the inhibition is primarily attributable to the S enantiomer (IC50, 0.0371 microM), which is approximately 200-fold more potent than the R enantiomer (IC50, 5.97 microM).  Carprofen binds to human serum albumin (HSA) by both fluorescence and equilibrium dialysis (ED) methods is characterized by two sets of association constants [K1 = 5.1 μM (fluorescence) and 3.7 μM (ED), K2 = 37 μM (fluorescence) and 13 μM (ED)]. Carprofen primarily binds to site II, the benzodiazepine site, while the low affinity site of carprofen is site I, the warfarin site, the carboxyl group of carprofen is found to play an important role especially in the high affinity binding of carprofen to HSA. 
|In vivo||Carprofen preoperatively has lower pain scores than the other groups, significantly so at 2 hours postextubation in the dogs. Carprofen (4 mg/kg) results in significant higher maximum plasma concentration, the area under the curve to the last data point, and area under the first moment curve up to the last data point in dogs.  Carprofen (4 mg/kg) provides slightly better pain relief than pethidine and produced less sedation in dogs. Carprofen provides good analgesia during the 18 hours the dogs are in hospital and no adverse side effects are observed.  Carprofen substantially increases the speed of lame birds, providing evidence that birds with moderate lameness suffer pain when they walk. |
-  Ricketts AP, et al. Am J Vet Res, 1998, 59(11), 1441-1446.
-  Rahman MH, et al. Biochem Pharmacol, 1993, 46(10), 1721-1731.
-  Lascelles BD, et al. Vet Surg, 1998, 27(6), 568-582.
|In vitro||DMSO||55 mg/mL (200.94 mM)|
|Ethanol||55 mg/mL (200.94 mM)|
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|% DMSO % % Tween 80 % ddH2O|
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