Size | Price | Stock | Qty |
---|---|---|---|
250mg |
|
||
500mg |
|
||
1g |
|
||
2g |
|
||
5g |
|
||
10g |
|
||
Other Sizes |
|
Purity: ≥98%
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.
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 |
|
||
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 |
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 |
|
|
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 (In Vitro) |
|
|||
---|---|---|---|---|
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. View More
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. |
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.
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.