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编 号：F753772
分子式：C20H14ClFN4OS
分子量：412.87
分子式：C20H14ClFN4OS
分子量：412.87
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CAS No: 2566522-50-5
产品详情
生物活性：
Antifungal agent 25 is a potent broad-spectrum antifungal agent. Antifungal agent 25 shows antifungal effect against Candida albicans and fluconazole-resistant strain of Candida albicans. Antifungal agent 25 stable metabolic property in vivo.
体内研究：
Antifungal agent 25 (2 mg/kg; i.v.) exhibits stable metabolic property in SD rats.Pharmacokinetic Parameters of Antifungal agent 25 in SD rats.dose(mg/kg)C0(ng/mL) T1/2(h)Vdss(L/kg) Cl (mL/min/kg) AUC0-last (ng·h/mL) AUC0-inf (ng·h/mL)
2 mg/kg482±1083.34±2.3710.3±3.1269.4±18.8483±1375.5±136
SD rats; 2 mg/kg; i.v..Animal Model:SD rats
Dosage:2 mg/kg
Administration: I.v.
Result:Exhibited stable metabolic property in SD rats.
体外研究：
Antifungal agent 25 (compound A31) shows antifungal effect with MIC values of 64 μg/mL for strain CaR (fluconazole-resistant strain of Candida albicans) and strain 17# (fluconazole and itraconazole resistant strain of Candida albicans), respectively.Antifungal agent 25 (0.015 mg/mL) blocks the biosynthesis of ergosterol by inhibiting the key enzyme lanosterol 14a-demethylase (CYP51).Antifungal agent 25 shows less likely to produce drug-drug interactions with IC50s of 4.47, 2.87, 1.04, 31.3, 10.1 μM for α-naphthoflavone (CYP1A2), sulfaphenazole (CYP2C9), ticlopidine (CYP2C19), quinidine (CYP2D6), and ketoconazole (CYP3A4), respectively.
Antifungal agent 25 is a potent broad-spectrum antifungal agent. Antifungal agent 25 shows antifungal effect against Candida albicans and fluconazole-resistant strain of Candida albicans. Antifungal agent 25 stable metabolic property in vivo.
体内研究：
Antifungal agent 25 (2 mg/kg; i.v.) exhibits stable metabolic property in SD rats.Pharmacokinetic Parameters of Antifungal agent 25 in SD rats.dose(mg/kg)C0(ng/mL) T1/2(h)Vdss(L/kg) Cl (mL/min/kg) AUC0-last (ng·h/mL) AUC0-inf (ng·h/mL)
2 mg/kg482±1083.34±2.3710.3±3.1269.4±18.8483±1375.5±136
SD rats; 2 mg/kg; i.v..Animal Model:SD rats
Dosage:2 mg/kg
Administration: I.v.
Result:Exhibited stable metabolic property in SD rats.
体外研究：
Antifungal agent 25 (compound A31) shows antifungal effect with MIC values of 64 μg/mL for strain CaR (fluconazole-resistant strain of Candida albicans) and strain 17# (fluconazole and itraconazole resistant strain of Candida albicans), respectively.Antifungal agent 25 (0.015 mg/mL) blocks the biosynthesis of ergosterol by inhibiting the key enzyme lanosterol 14a-demethylase (CYP51).Antifungal agent 25 shows less likely to produce drug-drug interactions with IC50s of 4.47, 2.87, 1.04, 31.3, 10.1 μM for α-naphthoflavone (CYP1A2), sulfaphenazole (CYP2C9), ticlopidine (CYP2C19), quinidine (CYP2D6), and ketoconazole (CYP3A4), respectively.
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