1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. VT-1598 tosylate

VT-1598 甲苯磺酸盐是一种口服有效、选择性的真菌抑制剂,靶向 CYP51。VT-1598 甲苯磺酸盐具有对白色念珠菌的抗真菌活性。

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VT-1598 tosylate Chemical Structure

VT-1598 tosylate Chemical Structure

CAS No. : 2089321-00-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1][2]. 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.

IC50 & Target

CYP51[1]

体外研究
(In Vitro)

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[1]
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[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

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[1]
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[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mice model of invasive candidiasis[1]
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[2]
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.
Clinical Trial
分子量

756.72

Formula

C38H28F4N6O5S

CAS 号
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.

纯度 & 产品资料
参考文献

VT-1598 tosylate 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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