Catalog No.S4136

For research use only.

Carprofen inhibits canine COX2 with IC50 of 30 nM.

Carprofen Chemical Structure

CAS No. 53716-49-7

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Biological Activity

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.
canine COX2 [1]
30 nM
In vitro

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). [1] 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. [2]

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. [3] 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. [4] Carprofen substantially increases the speed of lame birds, providing evidence that birds with moderate lameness suffer pain when they walk. [5]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 55 mg/mL
(200.94 mM)
Ethanol 55 mg/mL
(200.94 mM)
Water Insoluble

Chemical Information

Molecular Weight 273.71

C15 H12ClNO2

CAS No. 53716-49-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C1=CC2=C(C=C1)C3=C(N2)C=CC(=C3)Cl)C(=O)O

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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