VT-1598
Based on 1 Customer Validation
VT-1598 is an orally active and selective fungal inhibitor targeting CYP51. VT-1598 shows anti-fungal activity against Candida auris. 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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.86%
- No. CAS: 2089320-99-8
- Fòrmula: C31H20F4N6O2
- Peso molecular:584.52
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:100 C. auris isolates
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Concentration:0.015-8 μg/mL
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Incubation Time:24 hours
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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.
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Cell Line:28 Candida isolates obtained from mucosal sites of APECED patients
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Concentration:0.03125-0.125 μg/mL
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Incubation Time:24 hours
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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.
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].
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, 15, 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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2089320-99-8
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Appearance Solid
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Peso molecular 584.52
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Fòrmula C31H20F4N6O2
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Color Off-white to light yellow
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SMILES
N#CC1=CC=C(COC2=CC=C(C#CC3=CC=C(C(F)(F)[C@@](O)(C4=CC=C(F)C=C4F)CN5N=NN=C5)N=C3)C=C2)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (171.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7108 mL | 8.5540 mL | 17.1081 mL | 42.7701 mL |
| 5 mM | 0.3422 mL | 1.7108 mL | 3.4216 mL | 8.5540 mL | |
| 10 mM | 0.1711 mL | 0.8554 mL | 1.7108 mL | 4.2770 mL | |
| 15 mM | 0.1141 mL | 0.5703 mL | 1.1405 mL | 2.8513 mL | |
| 20 mM | 0.0855 mL | 0.4277 mL | 0.8554 mL | 2.1385 mL | |
| 25 mM | 0.0684 mL | 0.3422 mL | 0.6843 mL | 1.7108 mL | |
| 30 mM | 0.0570 mL | 0.2851 mL | 0.5703 mL | 1.4257 mL | |
| 40 mM | 0.0428 mL | 0.2139 mL | 0.4277 mL | 1.0693 mL | |
| 50 mM | 0.0342 mL | 0.1711 mL | 0.3422 mL | 0.8554 mL | |
| 60 mM | 0.0285 mL | 0.1426 mL | 0.2851 mL | 0.7128 mL | |
| 80 mM | 0.0214 mL | 0.1069 mL | 0.2139 mL | 0.5346 mL | |
| 100 mM | 0.0171 mL | 0.0855 mL | 0.1711 mL | 0.4277 mL |
VT-1598 Related Classifications
HY-123777 Related Classifications
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