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.
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- CAS No.: 852-19-7
- Formule: C16H16N4O2S
- Masse moléculaire:328.39
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Stockage:
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Activité biologique
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Chemical Information
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Activité biologique
Description
IC50 & Target
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CYP2C9 |
In Vitro
Sulfamethylphenazole (compound 16c) moderately inhibits Mycobacterium tuberculosis H37Rv, with an MIC of 15.38 μg/mL[1].
Sulfamethylphenazole (0.5 μM) inhibits CYP 2C9 by 45.0%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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.
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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.
Chemical Information
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CAS No. 852-19-7
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Masse moléculaire 328.39
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Formule C16H16N4O2S
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SMILES
O=S(NC1=CC(C)=NN1C2=CC=CC=C2)(C3=CC=C(N)C=C3)=O
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Synonyms
Sulfapyrazole; Vesulong
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Sulfamethylphenazole Related Classifications
HY-105828 Related Classifications
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