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编 号：F754206
分子式：C21H26Cl3NOS
分子量：446.86
分子式：C21H26Cl3NOS
分子量：446.86
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CAS No: 2640054-39-1
产品详情
生物活性：
Antifungal agent 22 (compound D16) is a potential and orally active antifungal agent for CM (cryptococcal meningitis), with an IC50 of 0.5 μg/mL. Antifungal agent 22 can penetrate the blood-brain barrier and kill the C. neoformans H99 cells by destroying the integrity of fungal cell membranes. Antifungal agent 22 shows selective anti-Cryptococcus activity with good metabolic stability and low cytotoxicity.
体内研究：
Antifungal agent 22 (D16) (15 mg/kg, Intragastrically, daily for 5 days) shows potent anti-Cryptococcal efficacy.Animal Model:ICR female mice (18-22 g, 4-6 weeks, tail vein injected with C. neoformans H99 cells)
Dosage:15 mg/kg
Administration:Intragastrically, daily for 5 days
Result:Showed potent anti-Cryptococcal efficacy, significantly reduced the number of C. neoformans H99 cells in the brain after 5 days, prolong the median survival time (14 days) of the infected mice at a dose of 15 mg/kg.
体外研究：
Antifungal agent 22 (compound D16) (0-1 μg/mL, 24 h) inhibits ergosterol biosynthesis, which results in stress-induced upregulation of ERG genes in C. neoformans H99.Antifungal agent 22 (0-8 μg/mL) effectively inhibits the growth of C. neoformans H99 (0-72 h), inhibits the formation of C. neoformans H99 biofilms in a concentration-dependent manner (24 h).Antifungal agent 22 (0-8 μg/mL, 48-72 h) shows selective anti-Cryptococcus activity, has a fungistatic effect.Antifungal agent 22 (0-100 μM, 48 h) shows low cytotoxicity against a human HUVEC cell line with an IC50 of 20.18 μM.
Antifungal agent 22 (compound D16) is a potential and orally active antifungal agent for CM (cryptococcal meningitis), with an IC50 of 0.5 μg/mL. Antifungal agent 22 can penetrate the blood-brain barrier and kill the C. neoformans H99 cells by destroying the integrity of fungal cell membranes. Antifungal agent 22 shows selective anti-Cryptococcus activity with good metabolic stability and low cytotoxicity.
体内研究：
Antifungal agent 22 (D16) (15 mg/kg, Intragastrically, daily for 5 days) shows potent anti-Cryptococcal efficacy.Animal Model:ICR female mice (18-22 g, 4-6 weeks, tail vein injected with C. neoformans H99 cells)
Dosage:15 mg/kg
Administration:Intragastrically, daily for 5 days
Result:Showed potent anti-Cryptococcal efficacy, significantly reduced the number of C. neoformans H99 cells in the brain after 5 days, prolong the median survival time (14 days) of the infected mice at a dose of 15 mg/kg.
体外研究：
Antifungal agent 22 (compound D16) (0-1 μg/mL, 24 h) inhibits ergosterol biosynthesis, which results in stress-induced upregulation of ERG genes in C. neoformans H99.Antifungal agent 22 (0-8 μg/mL) effectively inhibits the growth of C. neoformans H99 (0-72 h), inhibits the formation of C. neoformans H99 biofilms in a concentration-dependent manner (24 h).Antifungal agent 22 (0-8 μg/mL, 48-72 h) shows selective anti-Cryptococcus activity, has a fungistatic effect.Antifungal agent 22 (0-100 μM, 48 h) shows low cytotoxicity against a human HUVEC cell line with an IC50 of 20.18 μM.
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