Sulfamethylphenazole potassium
Sulfamethylphenazole potassium (Sulfapyrazole potassium; Vesulong potassium) is a long-acting sulfonamide antibacterial agent. Sulfamethylphenazole potassium maintains effective chemotherapeutic blood concentrations through the slow release of free sulfonamide from a protein-binding reservoir and can be used in combination with antibiotics such as Terramycin for bovine hemorrhagic septicemia. Sulfamethylphenazole potassium exhibits moderate antimycobacterial activity against Mycobacterium tuberculosis H37Rv (MIC = 15.38 μg/mL) and inhibitory activity against CYP 2C9. Sulfamethylphenazole potassium can be used in studies related to tuberculosis and hemorrhagic septicemia.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 18179-68-5
- 分子式: C16H16KN4O2S
- 分子量:367.49
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
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CYP2C9 |
体外実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female calves (Kalbinnen), 2-3 years of age[2]
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Dosage:10 mL/100 kg; 20 mL/100 kg; 30 mL/100 kg
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Administration:i.m.; single injection
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Result:10 mL/100 kg dose group: twenty-four hours after dosing, the mean total sulfonamide in whole blood was 0.8 mg/100 mL and the mean free sulfonamide was 0.1 mg/100 mL. This free level was below the chemotherapeutically active threshold (0.2-0.3 mg/100 mL whole blood) and did not maintain an effective blood concentration.
20 mL/100 kg dose group: twenty-four hours after dosing, the mean total sulfonamide in whole blood was 2.1 mg/100 mL and the mean free sulfonamide was 0.3 mg/100 mL. This free level reached the active threshold and sustained a chemotherapeutically effective concentration for at least 24 hours.
30 mL/100 kg dose group: twenty-four hours after dosing, the mean total sulfonamide in whole blood was 4.2 mg/100 mL and the mean free sulfonamide was 0.7 mg/100 mL. This exceeded the active threshold and represented supratherapeutic exposure.
A single intramuscular injection of 20 mL of the 20% test sulfonamide solution per 100 kg body weight was the optimal dosage to maintain a chemotherapeutically active free sulfonamide level for at least 24 hours in cattle.
化学情報
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CAS 番号 18179-68-5
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分子量 367.49
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分子式 C16H16KN4O2S
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SMILES
O=S(NC1=CC(C)=NN1C2=CC=CC=C2)(C3=CC=C(C=C3)N)=O.[K]
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別名
Sulfapyrazole potassium; Vesulong potassium
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Chen H, et al. The optimization and characterization of functionalized sulfonamides derived from sulfaphenazole against Mycobacterium tuberculosis with reduced CYP 2C9 inhibition. Bioorganic & medicinal chemistry letters. 2021 May 15;40:127924. [Content Brief]
[3]. Sheikh MA, Anzam M, Shakoori AR. Observations on haemorrhagic septicaemia in Pakistan livestock. Zentralbl Veterinarmed B. 1996 Jul;43(5):293-304. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Sulfamethylphenazole potassium 関連分類
HY-105828B 関連分類
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