| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 50mg | |||
| Other Sizes |
| Targets |
Piketoprofen is a COX inhibitor. Like other NSAIDs, it works by inhibiting the cyclooxygenase (COX) enzymes, thereby reducing the synthesis of prostaglandins, which are key mediators of inflammation and pain. Its amide form is a prodrug of a COX-2 inhibitor.
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|---|---|
| ln Vitro |
In vitro, Piketoprofen acts as a non-steroidal anti-inflammatory agent. Its activity is measured by its ability to inhibit COX enzymes and reduce prostaglandin production in cell-based assays.
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| ln Vivo |
In vivo, Piketoprofen is used topically to provide analgesic and anti-inflammatory effects. It is commonly applied as a cream or gel to relieve pain and reduce inflammation associated with conditions such as arthritis, musculoskeletal disorders, and postoperative pain.
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| Enzyme Assay |
The in vitro assay for Piketoprofen measures its ability to inhibit COX-1 and COX-2 enzyme activity. This is typically performed using a biochemical assay where the enzyme is incubated with arachidonic acid and the inhibitor, and the production of prostaglandins is measured.
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| Cell Assay |
In vitro cell-based assays are used to confirm its anti-inflammatory activity. Cells are stimulated with an inflammatory agent (e.g., LPS) in the presence of Piketoprofen, and the production of PGE2 is measured by ELISA. This confirms its ability to reduce prostaglandin synthesis in a cellular context.
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| Animal Protocol |
In vivo activity is evaluated in animal models of inflammation, such as the carrageenan-induced paw edema model. Topical application of the compound reduces paw swelling, demonstrating its local anti-inflammatory efficacy.
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| ADME/Pharmacokinetics |
As a topical drug, Piketoprofen is designed for localized delivery and has minimal systemic absorption. Its pharmacokinetic properties are characterized by high local concentrations at the site of application with low systemic exposure, reducing the risk of systemic side effects.
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| Toxicity/Toxicokinetics |
The topical formulation of Piketoprofen is generally well-tolerated. Local skin reactions, such as redness or itching, are the most common side effects. Systemic side effects are rare due to the low systemic absorption of the drug.
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| Additional Infomation |
Piketoprofen belongs to the benzophenone class of compounds.
Piketoprofen is a marketed drug in some countries for topical pain relief. It offers the advantage of localized treatment for musculoskeletal conditions with a lower risk of the gastrointestinal and cardiovascular side effects associated with oral NSAIDs. |
| Molecular Formula |
C22H20N2O2
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|---|---|
| Molecular Weight |
344.41
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| Exact Mass |
344.152
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| CAS # |
60576-13-8
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| Related CAS # |
59512-37-7 (HCl); 60576-13-8;
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| PubChem CID |
68801
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.195g/cm3
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| Boiling Point |
583.5ºC at 760 mmHg
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| Flash Point |
306.7ºC
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| Index of Refraction |
1.628
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| LogP |
4.436
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
26
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| Complexity |
487
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1C=CN=C(NC(C(C2C=CC=C(C(C3C=CC=CC=3)=O)C=2)C)=O)C=1
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| InChi Key |
ASFKKFRSMGBFRO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H20N2O2/c1-15-11-12-23-20(13-15)24-22(26)16(2)18-9-6-10-19(14-18)21(25)17-7-4-3-5-8-17/h3-14,16H,1-2H3,(H,23,24,26)
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| Chemical Name |
2-(3-benzoylphenyl)-N-(4-methylpyridin-2-yl)propanamide
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| Synonyms |
Calmatel Piketoprofen
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9035 mL | 14.5176 mL | 29.0352 mL | |
| 5 mM | 0.5807 mL | 2.9035 mL | 5.8070 mL | |
| 10 mM | 0.2904 mL | 1.4518 mL | 2.9035 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.
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