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

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.

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VT-1598 tosylate Chemical Structure

VT-1598 tosylate Chemical Structure

CAS No. : 2089321-00-4

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Description

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]

In Vitro

VT-1598 tosylate (0.015-8 μg/mL; 24 h) demonstrates in vitro activity against C. auris[1].
VT-1598 tosylate (0.03125-0.125 μg/mL; 24 h) shows highly effects in inhibiting the in vitro growth of clinical Candida isolates[2].

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

In Vivo

VT-1598 tosylate (oral gavage; 5, 15, and 50 mg/kg; once daily; 7 d) shows a significant and dose-dependent survival advantage for mice, and dose-dependent reductions in fungal burden in mice[1].
VT-1598 tosylate (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].

MedChemExpress (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
Molecular Weight

756.72

Formula

C38H28F4N6O5S

CAS No.
SMILES

O=S(O)(C1=CC=C(C=C1)C)=O.FC(F)(C2=CC=C(C=N2)C#CC3=CC=C(C=C3)OCC4=CC=C(C=C4)C#N)[C@@](O)(C5=C(C=C(C=C5)F)F)CN6C=NN=N6

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    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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VT-1598 tosylate
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HY-123777A
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