Xanthine oxidase-IN-24
Xanthine oxidase-IN-24 is an orally active mixed-type inhibitor of xanthine oxidase, with an IC50 of 0.051 μM and a Ki of 0.162 μM. Xanthine oxidase-IN-24 interacts with both free xanthine oxidase and the xanthine-xanthine oxidase complex, and reduces uric acid production in vivo. In a rat model of hyperuricemia induced by Potassium oxonate (HY-17511), Xanthine oxidase-IN-24 dose-dependently lowers serum uric acid levels, improves renal function-related biochemical parameters such as creatinine and urea nitrogen, and alleviates histopathological damage to liver and kidney tissues. Xanthine oxidase-IN-24 can be used in the research of hyperuricemia.
For research use only. We do not sell to patients.
- Formula: C26H32N6O3
- Molecular Weight:476.57
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
Xanthine oxidase-IN-24 (compound S40) effectively inhibits bovine milk xanthine oxidase in in vitro enzyme assays, with an IC50 of 0.051 μM; it acts as a mixed-type inhibitor of purified bovine xanthine oxidase, with a Ki value of 0.162 μM[1].
Xanthine oxidase-IN-24 can form highly stable and favorable interactions with xanthine oxidase, with an average binding free energy of -44.48 kcal/mol[1].
Xanthine oxidase-IN-24 exhibits excellent in vitro metabolic stability in rat liver microsomes, with a half-life of 131.5 min; it also demonstrates high in vitro stability in rat plasma under both incubation conditions of 37°C and 4°C[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUClast | Vd | CL | MRT |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 5.4 mg/kg | p.o. | 0.79 h | 1 h | 19.75 ng/mL | 19.25 ng·h/mL | 308.2 L/kg | 269.6 L/h/kg | 1.35 h |
In Vivo
Xanthine oxidase-IN-24 (8-32 mg/kg; p.o., once daily for 7 consecutive days) ameliorates renal and hepatic histopathological injuries associated with chronic hyperuricemia in rats in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rats (male, 6 weeks old, 180-220 g, Potassium oxonate-induced acute hyperuricemia model)[1]
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Dosage:8 mg/kg; 16 mg/kg; 32 mg/kg
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Administration:p.o.; single administration
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Result:Reduced serum uric acid levels at 2 h in a dose-dependent manner, with 22% reduction at 8 mg/kg, 48% reduction at 16 mg/kg, and 55% reduction at 32 mg/kg.
Achieved corresponding reductions in area under the serum uric acid curve (AUC0.5-2h) of 29.2%, 43.47%, and 46.74%, respectively.
Reduced serum xanthine oxidase activity in a dose-dependent manner by 5.85% at 8 mg/kg, 21.83% at 16 mg/kg, and 35.6% at 32 mg/kg.\nReduced serum creatinine levels relative to the model group in a dose-dependent manner, with a reduction of 8.87% at 8 mg/kg, 21.71% at 16 mg/kg, and 26.60% at 32 mg/kg.
Achieved corresponding reductions in serum blood urea nitrogen levels of 4.44%, 16.89%, and 29.00%, respectively.
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Animal Model:Sprague-Dawley rats (male, 6 weeks old, 180-220 g, Potassium oxonate-induced chronic hyperuricemia model)[1]
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Dosage:8 mg/kg; 16 mg/kg; 32 mg/kg
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Administration:p.o.; daily for 7 days
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Result:Attenuated histopathological damage in kidney and liver tissues in a dose-dependent manner, ameliorating marked renal tubular injury, interstitial alterations, renal lipid droplet accumulation, mild hepatic edema, and hepatic inflammatory cell infiltration observed in the untreated hyperuricemic model group.
Showed no obvious histopathological abnormalities in heart tissue across all groups.
Chemical Information
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Molecular Weight 476.57
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Formula C26H32N6O3
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SMILES
O=C(CC(C)(C)C)N1CCCC(COC2=C(N3C=NN=C3)C=C(NC(C4=CC=NC=C4)=O)C=C2)C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Xanthine oxidase-IN-24 Related Classifications
HY-189143 Related Classifications
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Keywords
- Xanthine oxidase-IN-24
- Xanthine Oxidase
- rat plasma
- hyperuricemia
- bovine xanthine oxidase
- rat liver microsomes
- potassium oxonate-induced acute hyperuricemic rats
- xanthine oxidase
- hepatic histopathological damage
- chronic hyperuricemia-associated renal
- normal rats
- bovine milk xanthine oxidase
- Inhibitor
- inhibitor
- inhibit