Sulfamethylphenazole
Sulfamethylphenazole (Sulfapyrazole; Vesulong) is a long-acting sulfonamide antibacterial agent. Sulfamethylphenazole 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 exhibits moderate antimycobacterial activity against Mycobacterium tuberculosis H37Rv (MIC = 15.38 μg/mL) and inhibitory activity against CYP 2C9. Sulfamethylphenazole can be used in studies related to tuberculosis and hemorrhagic septicemia.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 852-19-7
- 分子式: C16H16N4O2S
- 分子量:328.39
-
保管条件:
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]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
|
CYP2C9 |
In a field survey of hemorrhagic septicemia in cattle/buffaloes in Punjab, Pakistan, Sulfamethylphenazole combined with terramycin is preferred by 60% of veterinarians, while its single use is accepted by 30% of them. Moreover, it is only effective when administered in the early stage of the disease[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Female calves (Kalbinnen), 2-3 years of age[2]
-
Dosage:10 mL/100 kg; 20 mL/100 kg; 30 mL/100 kg
-
Administration:i.m.; single injection
-
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
-
CAS 番号 852-19-7
-
分子量 328.39
-
分子式 C16H16N4O2S
-
SMILES
O=S(NC1=CC(C)=NN1C2=CC=CC=C2)(C3=CC=C(N)C=C3)=O
-
別名
Sulfapyrazole; Vesulong
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
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 関連分類
HY-105828 関連分類
Powered by Bioz