2. Metabolic Enzyme/Protease
  3. Xanthine Oxidase
  4. Azapropazone

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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Azapropazone

Azapropazone Chemical Structure

CAS No. : 13539-59-8

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Azapropazone Related Antibodies

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Description

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[1][2][3].

In Vitro

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 Related Antibodies
In Vivo

Azapropazone (50-100 mg/kg; i.v.; 30 minutes before vascular occlusion, 5 minutes before vascular occlusion release, and 2.5 hours after vascular occlusion release) exerts significant cardiomyocyte protective effects on dogs with ischemia-reperfusion injury. It reduces the degree and scope of ischemia, limits the infarct size in myocardial regions with mild to moderate blood flow restriction, and has no effect on regions with severe blood flow restriction[1].
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.

Animal Model: Sprague-Dawley (female, 14-18 days post-disease induction)[2]
Dosage: 150 mg/kg/day (10-13 day treatment; ED50); 100 mg/kg/day (14 day treatment); 200 mg/kg/day (14 day treatment)
Administration: p.o.; 10-13 days; 14 days
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.
Molecular Weight

300.36

Formula

C16H20N4O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C(C(N2N1C(N(C)C)=NC3=CC=C(C=C32)C)=O)CCC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3293 mL 16.6467 mL 33.2934 mL
5 mM 0.6659 mL 3.3293 mL 6.6587 mL
View the 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.

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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.67%

SDS (251 KB)

COA (254 KB)

Handling Instructions (2659 KB)
References

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
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Azapropazone Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Azapropazone13539-59-8Xanthine OxidaseXOprostaglandin E2xanthine oxidaseinterleukin-1neutrophilgouty arthritisarticular cartilagesuperoxidemyocardial ischemia and reperfusion injuryadjuvant arthritisprostaglandin F2αInhibitorinhibitorinhibit

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