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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- CAS No.: 2089321-00-4
- Formule: C38H28F4N6O5S
- Masse moléculaire:756.72
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
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; 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.
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Animal Model:Mice model of invasive candidiasis[1]
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Dosage:5 mg/kg, 15 mg/kg, and 50 mg/kg
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Administration:Oral gavage; once daily; 7 days
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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]
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Dosage:3.2, 8, and 20 mg/kg
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Administration:Oral gavage; once daily; 4 days
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Result:Resulted in high concentrations in the plasma and tongues of Candida-infected mice.
Chemical Information
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CAS No. 2089321-00-4
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Masse moléculaire 756.72
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Formule C38H28F4N6O5S
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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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
VT-1598 tosylate Related Classifications
HY-123777A Related Classifications
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