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| ln Vitro |
Horse serum TxB2 and horse secretion PGE2 are inhibited by vedaprofen, with IC50 values of 9±5 and 630±148 ng/mL, respectively[1]. Vedaprofen has antibacterial properties and inhibits the β-subunit of DNA polymerase III in Escherichia coli [2]. The high E is for Vidaprofen. Affinity for coli SC binding (Ki=131 μM) [2].
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| ln Vivo |
Dog vidaprofen pharmacokinetic parameters [3]. Oral dose (mg/kg) tmax (h) Cmax (ng/mL) AUC0–48 h (h·ng/mL) AUC0–∞ (h·ng/mL) F0–∞ (%) 0.5 12.7±2.1 2739 ± 277 0.63±0.14 7090±1311 7650±1348 86±7. Intravenous dose (mg/kg) t1/2β (h) AUC0–48 h (h·ng/mL) AUC0–∞ (h·ng/mL) 0.5 16.8±2.2 8612±1135 9518±1223
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| References |
[1]. P Lees, et al. PK-PD integration and PK-PD modelling of nonsteroidal anti-inflammatory drugs: principles and applications in veterinary pharmacology. J Vet Pharmacol Ther. 2004 Dec;27(6):491-502.
[2]. Zhou Yin,et al. DNA replication is the target for the antibacterial effects of nonsteroidal anti-inflammatory drugs. Chem Biol. 2014 Apr 24;21(4):481-487. [3]. M Hoeijmakers, et al. The pharmacokinetics of Vedaprofen and its enantiomers in dogs after single and multiple dosing. J Vet Pharmacol Ther. 2005 Jun;28(3):305-12. |
| Additional Infomation |
2-(4-cyclohexyl-1-naphthyl)propanoic acid is a member of the class of naphthalenes that is propionic acid in which one of the alpha-hydrogens is replaced by a 4-cyclohexyl-1-naphthyl group. It is a monocarboxylic acid and a member of naphthalenes. It is functionally related to a propionic acid.
Drug Indication Reduction of inflammation and relief of pain associated with musculoskeletal disorders and soft-tissue lesions (traumatic injuries and surgical trauma). In cases of anticipated surgical trauma, Quadrisol can be given prophylactically at least three hours prior to elective surgery. , |
| Molecular Formula |
C19H22O2
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|---|---|
| Molecular Weight |
282.383
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| Exact Mass |
282.162
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| CAS # |
71109-09-6
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| Related CAS # |
Vedaprofen-d3;1185054-34-5
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| PubChem CID |
72158
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.132g/cm3
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| Boiling Point |
465.9ºC at 760 mmHg
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| Melting Point |
150ºC
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| Flash Point |
362.5ºC
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| Index of Refraction |
1.603
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| LogP |
5.075
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
21
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| Complexity |
359
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(c1ccc(c2c1cccc2)C3CCCCC3)C(=O)O
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| InChi Key |
VZUGVMQFWFVFBX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H22O2/c1-13(19(20)21)15-11-12-16(14-7-3-2-4-8-14)18-10-6-5-9-17(15)18/h5-6,9-14H,2-4,7-8H2,1H3,(H,20,21)
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| Chemical Name |
2-(4-cyclohexylnaphthalen-1-yl)propanoic acid
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| Synonyms |
PM-150; PM 150; Vedaprofen
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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 : ~50 mg/mL (~177.07 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.85 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 25.0 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: ≥ 2.5 mg/mL (8.85 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 25.0 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: ≥ 2.5 mg/mL (8.85 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 | 3.5413 mL | 17.7066 mL | 35.4133 mL | |
| 5 mM | 0.7083 mL | 3.5413 mL | 7.0827 mL | |
| 10 mM | 0.3541 mL | 1.7707 mL | 3.5413 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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