| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
Vedaprofen targets cyclooxygenase-1 (COX-1), the enzyme responsible for prostaglandin synthesis. By inhibiting COX-1, it reduces the production of prostaglandins, particularly thromboxane B₂ (TxB₂) in serum and prostaglandin E₂ (PGE₂) in exudate. The compound also inhibits the E. coli DNA polymerase III β-subunit (sliding clamp), blocking DNA replication and repair. It is a propionic acid derivative NSAID.
|
|---|---|
| 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].
In vitro, vedaprofen inhibits COX-1 and reduces prostaglandin H₂ synthesis. It inhibits E. coli sliding clamp with an IC₅₀ of 222 μM and Ki of 131 μM. Vedaprofen inhibits serum TxB₂ in horses with an IC₅₀ of 9 ng/mL and exudate PGE₂ with an IC₅₀ of 630 ng/mL. The compound is soluble in DMSO at 50 mg/mL (177.07 mM) and in ethanol at 10 mg/mL. |
| 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
In vivo, vedaprofen is rapidly absorbed (tₘₐₓ 0.63 h) and almost completely absorbed (bioavailability 86%) in Greyhound dogs following oral administration at 0.5 mg/kg. The terminal half-life is 16.8 h after intravenous administration and 12.7 h after oral administration. Vedaprofen does not accumulate in plasma. It is used clinically in veterinary medicine for pain and inflammation management in horses and dogs. |
| Enzyme Assay |
COX-1 inhibition assays are performed using purified COX-1 enzyme or cell-based systems. Enzyme activity is measured by prostaglandin production using ELISA or radioimmunoassay. Vedaprofen is tested at various concentrations, and IC₅₀ values are calculated. E. coli sliding clamp inhibition assays use purified β-subunit protein and DNA polymerase III activity measurements. Binding affinity (Ki) is determined using surface plasmon resonance or fluorescence-based assays.
|
| Cell Assay |
In vitro cellular assays use various cell lines to assess COX inhibition and anti-inflammatory activity. Cells are stimulated with inflammatory stimuli (e.g., LPS, arachidonic acid) and treated with vedaprofen at various concentrations. Prostaglandin production is measured by ELISA. Cell viability is assessed by MTT assay. The compound is dissolved in DMSO for stock solutions and diluted in culture media for cellular experiments.
|
| Animal Protocol |
In vivo efficacy is evaluated in animal models of inflammation and pain, including carrageenan-induced paw edema and adjuvant-induced arthritis models in rodents. Vedaprofen is administered orally or intravenously. In veterinary species (horses, dogs), clinical efficacy is assessed in musculoskeletal disorders. Endpoints include pain scores, lameness assessment, and inflammatory marker measurements. Pharmacokinetic studies are conducted in target animal species.
|
| ADME/Pharmacokinetics |
Vedaprofen has a molecular weight of 282.38 and molecular formula C₁₉H₂₂O₂ with CAS number 71109-09-6. Oral bioavailability in dogs is 86% with rapid absorption (tₘₐₓ 0.63 h). Terminal half-life is 16.8 h (i.v.) and 12.7 h (p.o.). The compound is highly protein-bound. It is metabolized in the liver and excreted primarily in urine and feces. It should be stored as powder at -20°C for up to 3 years or in solvent at -80°C for 1 year.
|
| Toxicity/Toxicokinetics |
As an NSAID, vedaprofen may cause gastrointestinal irritation, ulceration, and bleeding, particularly with long-term use or high doses. Renal and hepatic effects may occur. Hypersensitivity reactions are possible in sensitive individuals. In veterinary use, it should be used with caution in animals with pre-existing gastrointestinal, renal, or hepatic disease. The compound should not be used in pregnant or lactating animals unless specifically indicated.
|
| 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)propionic acid is a naphthalene compound, a derivative of propionic acid in which one α-hydrogen atom is replaced by a 4-cyclohexyl-1-naphthyl group. It is a monocarboxylic acid belonging to the naphthalene family, and its function is related to that of propionic acid.
Pharmacological Indications It is used to relieve inflammation and pain caused by musculoskeletal disorders and soft tissue injuries (traumatic and surgical trauma). For patients expected to undergo surgical trauma, Quadrisol may be administered prophylactically at least three hours before elective surgery. Vedaprofen (Quadrisol) is a veterinary NSAID used for the management of pain and inflammation in horses and dogs. It is a propionic acid derivative with COX-1 selectivity. The compound is administered orally or intravenously for acute and chronic musculoskeletal disorders, as well as for soft tissue injuries and surgical trauma. It may be administered prophylactically at least three hours before elective surgery. Vedaprofen is available in various formulations for veterinary use. |
| Molecular Formula |
C19H22O2
|
|---|---|
| Molecular Weight |
282.383
|
| Exact Mass |
282.162
|
| CAS # |
71109-09-6
|
| Related CAS # |
Vedaprofen-d3;1185054-34-5
|
| PubChem CID |
72158
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.132g/cm3
|
| Boiling Point |
465.9ºC at 760 mmHg
|
| Melting Point |
150ºC
|
| Flash Point |
362.5ºC
|
| Index of Refraction |
1.603
|
| LogP |
5.075
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
21
|
| Complexity |
359
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(c1ccc(c2c1cccc2)C3CCCCC3)C(=O)O
|
| InChi Key |
VZUGVMQFWFVFBX-UHFFFAOYSA-N
|
| 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)
|
| Chemical Name |
2-(4-cyclohexylnaphthalen-1-yl)propanoic acid
|
| Synonyms |
PM-150; PM 150; Vedaprofen
|
| HS Tariff Code |
2934.99.9001
|
| 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) |
DMSO : ~50 mg/mL (~177.07 mM)
|
|---|---|
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
