VT-1598

Research use only, not for human use.

VT-1598 is a potent, high-affinity, oral inhibitor of fungal sterol 14α-demethylase (CYP51B) with Kd of 13 nM.

VT-1598 is a potent, high-affinity, oral inhibitor of fungal sterol 14α-demethylase (CYP51B) with Kd of 13 nM; is more selective for fungal CYP51 than related human CYP enzymes such as CYP3A4; exhibits excellent potency against yeast, dermatophyte, and mold fungal pathogens.

Cell Viability Assay Cell Line:100?C. auris isolatesConcentration:0.015-8?μg/mL Incubation Time:24 hours Result:Showed MICs ranging from 0.03 to 8?μg/ mL against all isolates, with MIC50 and MIC90 values of 0.25 and 1?μg/mL, respectively.Cell Viability Assay 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 MIC50 and MIC90 values of 0.0625 and 0.125?mg/L, respectively.

Animal Model:Mice model of invasive candidiasis Dosage:5, 15, and 50?mg/kg Administration:Oral gavage; once daily; 7 daysResult: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.

VT1598

Microbiology/Virology

Fungal

Fungal

Infection

——

2089320-99-8

584.535

C31H20F4N6O2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (171.08 mM)

C1=CC(=CC=C1COC2=CC=C(C=C2)C#CC3=CN=C(C=C3)C(C(CN4C=NN=N4)(C5=C(C=C(C=C5)F)F)O)(F)F)C#N

(R)-4-((4-((6-(2-(2,4-difluorophenyl)-1,1-difluoro-2-hydroxy-3-(1H-tetrazol-1-yl)propyl)pyridin-3-yl)ethynyl)phenoxy)methyl)benzonitrile

(-20℃)

With Ice Pack

≥ 2 years