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编 号：F748780
分子式：C38H28F4N6O5S
分子量：756.72
分子式：C38H28F4N6O5S
分子量：756.72
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CAS No: 2089321-00-4
产品详情
生物活性：
VT-1598 tosylate is an orally active and selective fungal inhibitor targeting CYP51. VT-1598 tosylate shows anti-fungal activity against C. auris. VT-1598 (tosylate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
VT-1598 甲苯磺酸盐 (口服灌胃; 5, 15, and 50?mg/kg; 每天一次; 7 天) 处理小鼠，使其呈剂量依赖性的生存优势，VT-1598 还剂量依赖性降低小鼠体内的真菌负荷量。VT-1598 甲苯磺酸盐 (口服灌胃; 3.2, 8, and 20?mg/kg; 每天一次; 4 天) 在感染白色念珠菌 (C. albicans) 的 Act1 缺陷小鼠的血浆和舌中大量存在。Animal Model:Mice model of invasive candidiasis
Dosage:5 mg/kg, 15 mg/kg, and 50?mg/kg
Administration:Oral gavage; once daily; 7 days
Result:Observed median survival in the VT-1598 15 mg/kg and 50 mg/kg groups (15?days and >21?days, respectively) longer than the control group.Observed kidney fungal burden in mice treated with 15 mg/kg and 50 mg/kg doses (mean log10 CFU/g, 5.40 and 3.67, respectively) lower than the vehicle control group.Showed mean trough concentrations 1.55?μg/mL after 7?days of therapy in the 5 mg/kg group, 6.78?μg/mL in the 15 mg/kg group, and 14.2?μg/mL in the 50 mg/kg group.
Animal Model:Act1-deficient mice infected with C. albicans
Dosage:3.2, 8, and 20?mg/kg
Administration:Oral gavage; once daily; 4 days
Result:Resulted in high concentrations in the plasma and tongues of Candida-infected mice.
体外研究：
VT-1598 甲苯磺酸盐 (0.015-8?μg/mL; 24 h) 对临床念珠菌 (C. auris) 具有体外抑制活性。VT-1598 甲苯磺酸盐 (0.03125-0.125?μg/mL; 24 h) 对临床念珠菌 (C. auris) 的体外生长有显著抑制作用。
VT-1598 tosylate is an orally active and selective fungal inhibitor targeting CYP51. VT-1598 tosylate shows anti-fungal activity against C. auris. VT-1598 (tosylate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
VT-1598 甲苯磺酸盐 (口服灌胃; 5, 15, and 50?mg/kg; 每天一次; 7 天) 处理小鼠，使其呈剂量依赖性的生存优势，VT-1598 还剂量依赖性降低小鼠体内的真菌负荷量。VT-1598 甲苯磺酸盐 (口服灌胃; 3.2, 8, and 20?mg/kg; 每天一次; 4 天) 在感染白色念珠菌 (C. albicans) 的 Act1 缺陷小鼠的血浆和舌中大量存在。Animal Model:Mice model of invasive candidiasis
Dosage:5 mg/kg, 15 mg/kg, and 50?mg/kg
Administration:Oral gavage; once daily; 7 days
Result:Observed median survival in the VT-1598 15 mg/kg and 50 mg/kg groups (15?days and >21?days, respectively) longer than the control group.Observed kidney fungal burden in mice treated with 15 mg/kg and 50 mg/kg doses (mean log10 CFU/g, 5.40 and 3.67, respectively) lower than the vehicle control group.Showed mean trough concentrations 1.55?μg/mL after 7?days of therapy in the 5 mg/kg group, 6.78?μg/mL in the 15 mg/kg group, and 14.2?μg/mL in the 50 mg/kg group.
Animal Model:Act1-deficient mice infected with C. albicans
Dosage:3.2, 8, and 20?mg/kg
Administration:Oral gavage; once daily; 4 days
Result:Resulted in high concentrations in the plasma and tongues of Candida-infected mice.
体外研究：
VT-1598 甲苯磺酸盐 (0.015-8?μg/mL; 24 h) 对临床念珠菌 (C. auris) 具有体外抑制活性。VT-1598 甲苯磺酸盐 (0.03125-0.125?μg/mL; 24 h) 对临床念珠菌 (C. auris) 的体外生长有显著抑制作用。
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