CYP51/HDAC-IN-1 是一种有效的,具有口服活性的CYP51/HDAC双重抑制剂。CYP51/HDAC-IN-1 抑制重要的毒力因子并下调相关耐药基因的表达。CYP51/HDAC-IN-1 对热带念珠菌病和隐球菌性脑膜炎均有有效的治疗作用。
生物活性 | CYP51/HDAC-IN-1 is a potent, orally activeCYP51/HDACdual 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[1]. |
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体外研究 (In Vitro) | CYP51/HDAC-IN-1 (compound A5) exhibits the best inhibitory activity against bothCandida tropicalis (C. tropicalis)andCryptococcus neoformans (C. neoformans)with an MIC80of 0.5 μg/mL[1]. 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))[1]. CYP51/HDAC-IN-1 inhibits biofilm formation ofC. tropicalisandC. neoformansin a dose-dependent manner[1]. CYP51/HDAC-IN-1 reduces the virulence ofC. neoformansthrough down-regulating capsule-associated genes CAP10 and CAP60[1]. CYP51/HDAC-IN-1 increases the activity against FLC-resistantC. tropicalisby inhibits the overexpression of efflux pump genes, and down-regulated ERG11 gene in ergosterol biosynthetic pathway[1]. 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)[1].
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体内研究 (In Vivo) | 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)[1].
Animal Model: | Female ICR mice, 4-6 weeks, 18-20g (injection with C. tropicalis and C. neoformans
via tail vein)[1] | Dosage: | 20 mg/kg | Administration: | p.o.; once a day; 5 consecutive days | Result: | Reduced kidney fungal burden and brain fungal burden. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |