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编 号：F753430
分子式：C30H40F2N6O4
分子量：586.67
分子式：C30H40F2N6O4
分子量：586.67
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CAS No: 2502095-64-7
产品详情
生物活性：
CYP51/HDAC-IN-1 is a potent, orally active CYP51/HDAC dual inhibitor. CYP51/HDAC-IN-1 inhibits important virulence factors and down-regulated resistance-associated genes. CYP51/HDAC-IN-1 exhibits potent therapeutic effects for both tropical candidiasis and cryptococcal meningitis.
体内研究：
CYP51/HDAC-IN-1 (20 mg/kg; p.o.; once a day for 5 consecutive days) exhibits potent therapeutic effects for both tropical candidiasis and cryptococcal meningitis (CM).Animal Model:Female ICR mice, 4-6 weeks, 18-20g (injection with C. tropicalis and C. neoformansvia tail vein)
Dosage:20 mg/kg
Administration:p.o.; once a day; 5 consecutive days
Result:Reduced kidney fungal burden and brain fungal burden.
体外研究：
CYP51/HDAC-IN-1 (compound A5) exhibits the best inhibitory activity against both Candida tropicalis (C. tropicalis) and Cryptococcus neoformans (C. neoformans) with an MIC80 of 0.5 μg/mL.CYP51/HDAC-IN-1 (human umbilical vein endothelial cell line (HUVEC)) shows low toxicity to human normal cells (IC50= 5.9 μg/mL (10.36 μM)).CYP51/HDAC-IN-1 inhibits biofilm formation of C. tropicalis and C. neoformans in a dose-dependent manner.CYP51/HDAC-IN-1 reduces the virulence of C. neoformans through down-regulating capsule-associated genes CAP10 and CAP60.CYP51/HDAC-IN-1 increases the activity against FLC-resistant C. tropicalis by inhibits the overexpression of efflux pump genes, and down-regulated ERG11 gene in ergosterol biosynthetic pathway.CYP51/HDAC-IN-1 exhibits HDAC inhibitory activity (IC50=2.38 μM) and down-regulated HDAC genes (Rpd3, Hos1, Hos2, Clr61, Clr62, Hda1 and Hos3).
CYP51/HDAC-IN-1 is a potent, orally active CYP51/HDAC dual inhibitor. CYP51/HDAC-IN-1 inhibits important virulence factors and down-regulated resistance-associated genes. CYP51/HDAC-IN-1 exhibits potent therapeutic effects for both tropical candidiasis and cryptococcal meningitis.
体内研究：
CYP51/HDAC-IN-1 (20 mg/kg; p.o.; once a day for 5 consecutive days) exhibits potent therapeutic effects for both tropical candidiasis and cryptococcal meningitis (CM).Animal Model:Female ICR mice, 4-6 weeks, 18-20g (injection with C. tropicalis and C. neoformansvia tail vein)
Dosage:20 mg/kg
Administration:p.o.; once a day; 5 consecutive days
Result:Reduced kidney fungal burden and brain fungal burden.
体外研究：
CYP51/HDAC-IN-1 (compound A5) exhibits the best inhibitory activity against both Candida tropicalis (C. tropicalis) and Cryptococcus neoformans (C. neoformans) with an MIC80 of 0.5 μg/mL.CYP51/HDAC-IN-1 (human umbilical vein endothelial cell line (HUVEC)) shows low toxicity to human normal cells (IC50= 5.9 μg/mL (10.36 μM)).CYP51/HDAC-IN-1 inhibits biofilm formation of C. tropicalis and C. neoformans in a dose-dependent manner.CYP51/HDAC-IN-1 reduces the virulence of C. neoformans through down-regulating capsule-associated genes CAP10 and CAP60.CYP51/HDAC-IN-1 increases the activity against FLC-resistant C. tropicalis by inhibits the overexpression of efflux pump genes, and down-regulated ERG11 gene in ergosterol biosynthetic pathway.CYP51/HDAC-IN-1 exhibits HDAC inhibitory activity (IC50=2.38 μM) and down-regulated HDAC genes (Rpd3, Hos1, Hos2, Clr61, Clr62, Hda1 and Hos3).
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