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    InvivoChem Cat #: V1074
    CAS #: 53716-49-7Purity ≥98%

    Description: Carprofen (Rimadyl; Ro-205720; C 5720; quellin; Novox; Imafen; Rovera), a nonsteroid anti-inflammatory drug (NSAID), is a potent and multi-target FAAH/COX inhibitor with potential anti-inflammatory activity. It inhibits COX-2, COX-1 and FAAH with IC50s of 3.9 μM, 22.3 μM and 78.6 μM, respectively. Veterinarians prescribe it as a supportive treatment for various conditions in animals, is a COX2 inhibitor that inhibits canine COX2 with IC50 of 30 nM. 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). It acts as a multi-target FAAH/COX inhibitor, with IC50s of 3.9 μM, 22.3 μM and 78.6 μM for COX-2, COX-1 and FAAH, respectively.

    References: Am J Vet Res. 1998 Nov;59(11):1441-6; Vet Surg. 1998 Nov-Dec;27(6):568-82.

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    Molecular Weight (MW)273.71 
    FormulaC15 H12ClNO2 
    CAS No.53716-49-7 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 55 mg/mL (200.9 mM)
    Water: <1 mg/mL
    Ethanol: 55 mg/mL (200.9 mM)
    Other infoChemical Name: 2-(6-chloro-9H-carbazol-2-yl)propanoic acid
    InChi Code: InChI=1S/C15H12ClNO2/c1-8(15(18)19)9-2-4-11-12-7-10(16)3-5-13(12)17-14(11)6-9/h2-8,17H,1H3,(H,18,19)
    SMILES Code: CC(C1=CC2=C(C=C1)C3=C(N2)C=CC(=C3)Cl)C(=O)O 
    SynonymsRo205720; C-5720; C5720; Carprofen; Imadyl; Rimadyl; Ridamyl; Ro 20-5720; Ro 205720; C 5720; Imadyl; quellin; Novox; Imafen; Rovera

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    In Vitro

    In vitro activity: 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.

    Cell Assay: Cruciate ligament cells are used and incubated with DMEM supplemented with 10% FCS for 24 hours to synchronize cell cycles. The cell cultures are then preincubated without (control) or with a nonselective COX inhibitor (acetylsalicylic acid) or a preferential COX-2 inhibitor (Carprofen, meloxicam, or robenacoxib) to ssess whether NSAIDs prevented apoptosis when the cells are subsequently incubated with SNP. For all cell cultures except those designated as controls, 1 of 3 concentrations of 1 of the 4 NSAIDs (10, 100, or 200 µg of acetylsalicylic acid/mL; 0.1, 1, or 10 µg of Carprofend/mL; 0.1, 1, or 10 µg of meloxicame/mL; or 0.1, 1, or 10 µg of robenacoxibf/mL) is added to the culture media of each cell culture, and the cells are incubated for 2 hours.

    In VivoCarprofen 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.  
    Animal modelDogs
    Formulation & DosageEach dog receives Carprofen (2.2 mg/kg, PO, q 12 h), deracoxib (2 mg/kg, PO, q 24 h), or etodolac (10 to 15 mg/kg, PO, q 24 h) for 10 days in a crossover design with a 30- to 60-day washout period between treatments. On days 0, 3, and 10 of each treatment period, blood is collected for evaluation of TXB2 and PGE2 concentrations. In addition, anesthesia is induced with propofol (4 mg/kg) and maintained with isoflurane. Synovial fluid is collected from both stifle joints by use of a standard arthrocentesis technique for evaluation of PGE2 concentrations. Gastroscopy is performed during each anesthetic episode, and 3 to 6 endoscopic biopsy specimens are collected from the gastric antrum for evaluation of PGE1 and PGE2 synthesis. On day 0 for each dog, a gastric biopsy specimen is placed into a Campylobacter-like organism test kit and evaluated for up to 24 hours for Helicobacter spp. Stained slides (H&E) of gastric biopsy specimens are also evaluated for the presence of underlying inflammation
    ReferencesAm J Vet Res. 1998 Nov;59(11):1441-6; Vet Surg. 1998 Nov-Dec;27(6):568-82; Am J Vet Res. 2005 May;66(5):812-7.

    These protocols are for reference only. InvivoChem does not independently validate these methods.


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