Vedaprofen
Based on 1 Customer Validation
Vedaprofen (Quadrisol) is a COX-1 selective nonsteroidal anti-inflammatory agent (NSAID) for serum TxB2 and exudate PGE2 inhibition . Vedaprofen is a Escherichia coli (E. coli) sliding clamp (SC) inhibitor with the IC50 of 222 μM.
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- Purity: 98.73%
- CAS No.: 71109-09-6
- 화학식: C19H22O2
- 분자량:282.38
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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COX-1 |
Vedaprofen inhibits horse serum TxB2 and horse exudate PGE2 with IC50s of 9±5 and 630±148 ng/mL, respectively[1]. Vedaprofen inhibit the E. coli DNA polymerase III β subunit with antibacterial potency[2]. Vedaprofen shows high E. coli SC binding affinity (Ki=131 μM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| 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 |
| Oral dose (mg/kg) | t1/2β (h) | Cmax (ng/mL) | tmax (h) | 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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 71109-09-6
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Appearance Solid
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분자량 282.38
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화학식 C19H22O2
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Color White to off-white
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SMILES
CC(C1=CC=C(C2CCCCC2)C3=C1C=CC=C3)C(O)=O
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Synonyms
Quadrisol; CERM 10202; PM 150
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 50 mg/mL (177.07 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.85 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.85 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.5413 mL | 17.7066 mL | 35.4133 mL | 88.5332 mL |
| 5 mM | 0.7083 mL | 3.5413 mL | 7.0827 mL | 17.7066 mL | |
| 10 mM | 0.3541 mL | 1.7707 mL | 3.5413 mL | 8.8533 mL | |
| 15 mM | 0.2361 mL | 1.1804 mL | 2.3609 mL | 5.9022 mL | |
| 20 mM | 0.1771 mL | 0.8853 mL | 1.7707 mL | 4.4267 mL | |
| 25 mM | 0.1417 mL | 0.7083 mL | 1.4165 mL | 3.5413 mL | |
| 30 mM | 0.1180 mL | 0.5902 mL | 1.1804 mL | 2.9511 mL | |
| 40 mM | 0.0885 mL | 0.4427 mL | 0.8853 mL | 2.2133 mL | |
| 50 mM | 0.0708 mL | 0.3541 mL | 0.7083 mL | 1.7707 mL | |
| 60 mM | 0.0590 mL | 0.2951 mL | 0.5902 mL | 1.4756 mL | |
| 80 mM | 0.0443 mL | 0.2213 mL | 0.4427 mL | 1.1067 mL | |
| 100 mM | 0.0354 mL | 0.1771 mL | 0.3541 mL | 0.8853 mL |