| Identification | Back Directory | [Name]
VT-1598 | [CAS]
2089320-99-8 | [Synonyms]
VT-1598
Benzonitrile, 4-[[4-[2-[6-[(2R)-2-(2,4-difluorophenyl)-1,1-difluoro-2-hydroxy-3-(1H-tetrazol-1-yl)propyl]-3-pyridinyl]ethynyl]phenoxy]methyl]- | [Molecular Formula]
C31H20F4N6O2 | [MOL File]
2089320-99-8.mol | [Molecular Weight]
584.52 |
| Hazard Information | Back Directory | [Uses]
VT-1598 is an orally active and selective fungal inhibitor targeting CYP51. VT-1598 shows anti-fungal activity against Candida auris[1][2]. VT-1598 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. | [in vivo]
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; 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.
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| 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. |
| [References]
[1] Nathan P Wiederhold, et al. The Fungal Cyp51-Specific Inhibitor VT-1598 Demonstrates In Vitro and In Vivo Activity against Candida auris. Antimicrob Agents Chemother. 2019 Feb 26;63(3):e02233-18. DOI:10.1128/AAC.02233-18
[2] Timothy J Break, et al. VT-1598 inhibits the in vitro growth of mucosal Candida strains and protects against fluconazole-susceptible and -resistant oral candidiasis in IL-17 signalling-deficient mice. J Antimicrob Chemother. 2018 Aug 1;73(8):2089-2094. DOI:10.1093/jac/dky170 |
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| Company Name: |
DC Chemicals
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| Tel: |
021-58447131 13564518121 |
| Website: |
www.chemicalbook.com/showsupplierproductslist927327/0_en.htm |
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