Carprofen

Alias: Ro205720; C-5720;Ro 205720;C5720; Carprofen; Imadyl; Rimadyl; Ridamyl; Ro 20-5720; C 5720; Imadyl; quellin; Novox; Imafen; Rovera
Cat No.:V1074 Purity: ≥98%
Carprofen (Rimadyl; Ro-205720; C 5720; quellin; Novox; Imafen; Rovera), a nonsteroid anti-inflammatory drug (NSAID), isa potent and multi-targetFAAH/COXinhibitor with potential anti-inflammatory activity.
Carprofen Chemical Structure CAS No.: 53716-49-7
Product category: COX
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
250mg
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1g
2g
5g
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Other Forms of Carprofen:

  • Carprofen-d3 (Carprofen d3)
  • Carprofen-13C,d3 (Carprofen-13C,d3; Carprofen-13C,d3; Carzoprofen-13C,d3)
Official Supplier of:
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Top Publications Citing lnvivochem Products
InvivoChem's Carprofen has been cited by 2 publications
Purity & Quality Control Documentation

Purity: ≥98%

Product 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.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Compound 1, or carprofen, is a non-steroidal anti-inflammatory drug. The IC50 values for COX-2, COX, and FAAH are 3.9 μM, 22.3 μM, and 78.6 μM-1, respectively, as a multi-target inhibitor of FAAH/COX. In CCL and CaCL cells, carprofen (10 μg/mL) has cytoprotective properties and lowers both cell apoptosis. When compared to the corresponding CCL or CaCL controls, PGE2 concentrations were not significantly increased by carprofen (10 μg/mL) [2].
ln Vivo
On days 3 and 10, carprofen (2.2 mg/kg, po) dramatically lowered the levels of PGE2 in canine blood. On day 3, carprofen similarly decreased the synthesis of PGE2 in the stomach; however, by day 10, the inhibition was not as great. Moreover, on days 3 and 10, it was demonstrated that carprofen had no effect on the synthesis of stomach PGE1 in dogs [3].
Animal Protocol
Each 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
Dogs
References
[1]. Favia AD, et al. Identification and characterization of carprofen as a multitarget fatty acid amide hydrolase/cyclooxygenase inhibitor. J Med Chem. 2012 Oct 25;55(20):8807-26.
[2]. Waldherr K, et al. In vitro cytoprotective effects of acetylsalicylic acid, carprofen, meloxicam, or robenacoxib against apoptosis induced by sodium nitroprusside in canine cruciate ligament cells. Am J Vet Res. 2012 Nov;73(11):1752-8.
[3]. Sessions JK, et al. In vivo effects of carprofen, deracoxib, and etodolac on prostanoid production in blood, gastric mucosa, and synovial fluid in dogs with chronic osteoarthritis. Am J Vet Res. 2005 May;66(5):812-7
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C15H12CLNO2
Molecular Weight
273.71
CAS #
53716-49-7
Related CAS #
Carprofen-d3;1173019-42-5;Carprofen-13C,d3;2012598-34-2
SMILES
ClC1C([H])=C([H])C2=C(C=1[H])C1C([H])=C([H])C(=C([H])C=1N2[H])C([H])(C(=O)O[H])C([H])([H])[H]
InChi Key
PUXBGTOOZJQSKH-UHFFFAOYSA-N
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)
Chemical Name
2-(6-chloro-9H-carbazol-2-yl)propanoic acid
Synonyms
Ro205720; C-5720;Ro 205720;C5720; Carprofen; Imadyl; Rimadyl; Ridamyl; Ro 20-5720; C 5720; Imadyl; quellin; Novox; Imafen; Rovera
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO:55 mg/mL (200.9 mM)
Water:<1 mg/mL
Ethanol:55 mg/mL (200.9 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.60 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.08 mg/mL (7.60 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (7.60 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.6535 mL 18.2675 mL 36.5350 mL
5 mM 0.7307 mL 3.6535 mL 7.3070 mL
10 mM 0.3654 mL 1.8268 mL 3.6535 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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