| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
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| ln Vitro |
S-(+)-Ketoprofen (compound 1) has an IC50 of 1.9 nM for COX-1 and 27 nM for COX-2, making it a strong inhibitor of both COXs [1].
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|---|---|
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
After oral ingestion, the Dexketoprofen onset of action is within 30 minutes. The plasma half-life of Dexketoprofen is about 4-6 hours. The Cmax is about 30 minutes Approximately 70 to 80% of the ingested dose is recovered in the urine during the first 12 hours post-ingestion, mainly as the acyl-conjugated form of the drug. <0.25 L/kg Mainly cleared via glucuronide conjugation and followed by renal excretion, mainly unchanged. Metabolism / Metabolites Dexketoprofen is highly lipophilic, and is metabolized in the liver by glucuronidation. In one study, after oral administration of 25 mg of dexketoprofen to young healthy adults, Tmax was approximately 30 min for a Cmax of 3.7 ± 0.72 mg/l. Dexketoprofen trometamol is metabolized by the hepatic cytochrome P450 enzymes (CYP2C8 and CYP2C9). Dexketoprofen trometamol has a number of metabolites, with hydroxyl derivatives making up the greatest volume. In humans, hydroxylation plays a minor role. Dexketoprofen is primarily conjugated to an acyl-glucuronide Biological Half-Life 1.65 h |
| Toxicity/Toxicokinetics |
Protein Binding
Highly protein bound. |
| References | |
| Additional Infomation |
Dexketoprofen is a monocarboxylic acid that is (S)-hydratropic acid substituted at position 3 on the phenyl ring by a benzoyl group. A cyclooxygenase inhibitor, it is used to relieve short-term pain, such as muscular pain, dental pain and dysmenorrhoea. It has a role as a non-steroidal anti-inflammatory drug, a cyclooxygenase 1 inhibitor, a cyclooxygenase 2 inhibitor and a non-narcotic analgesic. It is a monocarboxylic acid and a member of benzophenones. It is functionally related to a (S)-hydratropic acid.
Dexketoprofen is a non-steroidal anti-inflammatory drug. It is available in the various countries in Europe, Asia and Latin America. It has analgesic, antipyretic and anti-inflammatory properties. Drug Indication For short-term treatment of mild to moderate pain, including dysmenorrhoea, musculoskeletal pain and toothache. Mechanism of Action It is a non-steroidal anti-inflammatory drug (NSAID) that reduces prostaglandin synthesis via inhibition of cyclooxygenase pathway (both COX-1 and COX-2) activity. Pharmacodynamics This drug is an isomer of ketoprofen. Dexketoprofen a propionic acid derivative with analgesic, anti-inflammatory, and antipyretic properties. |
| Molecular Formula |
C₁₆H₁₄O₃
|
|---|---|
| Molecular Weight |
254.28
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| Exact Mass |
254.094
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| CAS # |
22161-81-5
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| Related CAS # |
Ketoprofen;22071-15-4;Dexketoprofen (trometamol);156604-79-4
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| PubChem CID |
667550
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| Appearance |
White to off-white solid powder
|
| Density |
1.2±0.1 g/cm3
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| Boiling Point |
431.3±28.0 °C at 760 mmHg
|
| Melting Point |
75-78ºC(lit.)
|
| Flash Point |
228.8±20.5 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
|
| Index of Refraction |
1.592
|
| LogP |
2.81
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| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
|
| Heavy Atom Count |
19
|
| Complexity |
331
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C[C@@H](C1=CC(=CC=C1)C(=O)C2=CC=CC=C2)C(=O)O
|
| InChi Key |
DKYWVDODHFEZIM-NSHDSACASA-N
|
| InChi Code |
InChI=1S/C16H14O3/c1-11(16(18)19)13-8-5-9-14(10-13)15(17)12-6-3-2-4-7-12/h2-11H,1H3,(H,18,19)/t11-/m0/s1
|
| Chemical Name |
Benzeneacetic acid, 3-benzoyl-alpha-methyl-, (S)-
|
| Synonyms |
(S)-Ketoprofen Dexketoprofen (S)-(+)-Ketoprofen
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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) |
DMSO : ~100 mg/mL (~393.27 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.18 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 (8.18 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 (8.18 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 | 3.9327 mL | 19.6634 mL | 39.3267 mL | |
| 5 mM | 0.7865 mL | 3.9327 mL | 7.8653 mL | |
| 10 mM | 0.3933 mL | 1.9663 mL | 3.9327 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.
Parecoxib vs. Dexketoprofen for the Management of Pain After Cesarean Section.
CTID: NCT04847024
Phase: N/A Status: Completed
Date: 2021-10-11
Products are for research use only; We do not sell to patients
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