Azapropazone
Based on 1 Customer Validation
Azapropazone is an orally active nonsteroidal anti-inflammatory agent. Azapropazone inhibits Xanthine oxidase activity with an IC50 of 70-140 μg/mL. Azapropazone exerts significant cardiomyocyte protective effects on dogs with ischemia-reperfusion injury. Azapropazone reduces arthritis. Azapropazone inhibits Adrenaline-induced platelet aggregation. Azapropazone can be used for the research of myocardial ischemia and reperfusion injury, adjuvant arthritis, and gouty arthritis.
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- Pureté: 99.67%
- CAS No.: 13539-59-8
- Formule: C16H20N4O2
- Masse moléculaire:300.36
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Azapropazone (70-140 μg/mL) inhibits xanthine oxidase activity in vitro with an IC50 of 70-140 μg/mL[1].
Azapropazone (40-400 μg/mL) inhibits multiple neutrophil functions (migration, aggregation)[1].
Azapropazone (10-200 μM; 10 min) potently inhibits superoxide anion generation by human PMNs stimulated with polyhistidine or TPA (half-maximal inhibition at ~15 μM) but not by histone-coated streptococci with cytochalasin B[2].
Azapropazone (5 μM; 1-5 min before or concurrent with stimulus addition) inhibits adrenaline-induced human platelet aggregation but has no effect on ADP- or thrombin-induced aggregation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Azapropazone (150-200 mg/kg; p.o.; 10-14 days) significantly reduces joint swelling, cartilage damage and clinical disease activity in rats with established adjuvant-induced arthritis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (female, 14-18 days post-disease induction)[2]
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Dosage:150 mg/kg/day (10-13 day treatment; ED50); 100 mg/kg/day (14 day treatment); 200 mg/kg/day (14 day treatment)
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Administration:p.o.; 10-13 days; 14 days
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Result:Produced a significant reduction in rear-paw and ankle swelling, comparable to standard NSAIDs.
Reduced cartilage destruction from a control score of 3.2 to 1.2.
Reduced periostitis/new bone growth from a control score of 4.0 to 2.8.
Reduced pannus formation from a control score of 4.0 to 2.8.
Resulted in an overall clinical disease activity score of 2.3 ± 0.5 (mean ± s.d.) compared to 0.0 for controls.
Showed no significant improvement in body weight.
Established an ED50 of 150 mg/kg/day after 14 days of treatment.
Showed no differences in efficacy between once-daily and divided-daily administration of 100 or 200 mg/kg/day.
Chemical Information
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CAS No. 13539-59-8
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Appearance Solid
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Masse moléculaire 300.36
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Formule C16H20N4O2
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Color White to off-white
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SMILES
O=C1C(C(N2N1C(N(C)C)=NC3=CC=C(C=C32)C)=O)CCC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 125 mg/mL (416.17 mM; Need ultrasonic; 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)
Pureté et documentation
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Fiche technique (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Mousa SA, et al. Myocardial cytoprotective efficacy of azapropazone in a canine heart model of regional ischemia and reperfusion. J Cardiovasc Pharmacol. 1989;14(4):542-548. [Content Brief]
[2]. Rainsford KD, et al. Comparative effects of azapropazone on cellular events at inflamed sites. Influence on joint pathology in arthritic rats, leucocyte superoxide and eicosanoid production, platelet aggregation, synthesis of cartilage proteoglycans, synovial production and actions of interleukin-1 in cartilage resorption correlated with drug uptake into cartilage in-vitro. J Pharm Pharmacol. 1989;41(5):322-330. [Content Brief]
[3]. Mackin WM, et al. Inhibition of rat neutrophil functional responses by azapropazone, an anti-gout drug. Biochem Pharmacol. 1986;35(6):917-922. [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 | 3.3293 mL | 16.6467 mL | 33.2934 mL | 83.2335 mL |
| 5 mM | 0.6659 mL | 3.3293 mL | 6.6587 mL | 16.6467 mL | |
| 10 mM | 0.3329 mL | 1.6647 mL | 3.3293 mL | 8.3233 mL | |
| 15 mM | 0.2220 mL | 1.1098 mL | 2.2196 mL | 5.5489 mL | |
| 20 mM | 0.1665 mL | 0.8323 mL | 1.6647 mL | 4.1617 mL | |
| 25 mM | 0.1332 mL | 0.6659 mL | 1.3317 mL | 3.3293 mL | |
| 30 mM | 0.1110 mL | 0.5549 mL | 1.1098 mL | 2.7744 mL | |
| 40 mM | 0.0832 mL | 0.4162 mL | 0.8323 mL | 2.0808 mL | |
| 50 mM | 0.0666 mL | 0.3329 mL | 0.6659 mL | 1.6647 mL | |
| 60 mM | 0.0555 mL | 0.2774 mL | 0.5549 mL | 1.3872 mL | |
| 80 mM | 0.0416 mL | 0.2081 mL | 0.4162 mL | 1.0404 mL | |
| 100 mM | 0.0333 mL | 0.1665 mL | 0.3329 mL | 0.8323 mL |
Azapropazone Related Classifications
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