VT-1598 是一种具有口服活性的、新型的、选择性的fungal CYP51抑制剂。VT-1598 具有对白色念珠菌的抗真菌活性。

VT-1598 is an orally active, novel and selective fungal CYP51 inhibitor. VT-1598 shows anti-fungal activity against Candida auris [1] [2].

VT-1598 (0.015-8 μg/mL; 24 h) demonstrates in vitro activity against C. auris [1]. VT-1598 (0.03125-0.125 μg/mL; 24 h) shows highly effects in inhibiting the in vitro growth of clinical Candida isolates [2]. Cell Viability Assay [1] Cell Line: 100 C. auris isolates Concentration: 0.015-8 μg/mL Incubation Time: 24 hours Result: Showed MICs ranging from 0.03 to 8 μg/ mL against all isolates, with MIC 50 and MIC 90 values of 0.25 and 1 μg/mL, respectively. Cell Viability Assay [2] Cell Line: 28 Candida isolates obtained from mucosal sites of APECED patients Concentration: 0.03125-0.125 μg/mL Incubation Time: 24 hours Result: Demonstrated potent in vitro activity against all 28 isolates (MIC range=0.03125-0.125 mg/L), with the MIC 50 and MIC 90 values of 0.0625 and 0.125 mg/L, respectively.

VT-1598 (oral gavage; 5, 15, and 50 mg/kg; once daily; 7 d) treatment shows a significant and dose-dependent survival advantage, and dose-dependent reductions in fungal burden [1]. VT-1598 (oral gavage; 3.2, 8, and 20 mg/kg; once daily; 4 d) is present to a great extent in the plasma and tongue after oral administration in Act1-deficient mice infected with C. albicans [2]. Animal Model: Mice model of invasive candidiasis [1] Dosage: 5, 15, and 50 mg/kg Administration: Oral gavage; 5, 15, and 50 mg/kg; 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 log 10 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; 3.2, 8, and 20 mg/kg; once daily; 4 days Result: Resulted in high concentrations in the plasma and tongues of Candida-infected mice.

2089320-99-8

C31H20F4N6O2

584.52

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years