Antifungal agent 22
Antifungal agent 22 (compound D16) is a potential and orally active antifungal agent for CM (cryptococcal meningitis), with an IC50 of 0.5 μg/mL. Antifungal agent 22 can penetrate the blood-brain barrier and kill the C. neoformans H99 cells by destroying the integrity of fungal cell membranes. Antifungal agent 22 shows selective anti-Cryptococcus activity with good metabolic stability and low cytotoxicity.
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- CAS. Nr.: 2640054-39-1
- Formel: C21H26Cl3NOS
- Molecular Weight:446.86
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
IC50: 0.5 μg/mL (Fungal)[1].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HUVEC | IC50 |
20.18 μM
Compound: D16
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Cytotoxicity against HUVEC cells
Cytotoxicity against HUVEC cells
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[PMID: 35253435] |
In Vitro
Antifungal agent 22 (compound D16) (0-1 μg/mL, 24 h) inhibits ergosterol biosynthesis, which results in stress-induced upregulation of ERG genes in C. neoformans H99[1].
Antifungal agent 22 (0-8 μg/mL) effectively inhibits the growth of C. neoformans H99 (0-72 h), inhibits the formation of C. neoformans H99 biofilms in a concentration-dependent manner (24 h)[1].
Antifungal agent 22 (0-8 μg/mL, 48-72 h) shows selective anti-Cryptococcus activity, has a fungistatic effect[1].
Antifungal agent 22 (0-100 μM, 48 h) shows low cytotoxicity against a human HUVEC cell line with an IC50 of 20.18 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:C. neoformans H99 cells[1]
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Concentration:0, 1, 2, 4, 8 μg/mL
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Incubation Time:0, 4, 8, 12, 24, 48, and 72 h
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Result:Almost completely inhibited the growth of C. neoformans H99 at 8 μg/mL, remained at nearly 100% inhibition rate after 72 h, had minimum fungicidal concentrations of 8 μg/mL.
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Cell Line:Fungal cells (RPMI 1640 medium)[1]
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Concentration:0, 0.5, 1, 2, 4, 8 μg/mL
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Incubation Time:48, 72 h
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Result:Showed selective anti-Cryptococcus activity, with IC50 range of 0.06-2 μg/mL and a MIC50 value (average IC50 values) of 0.62 μg/mL.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR female mice (18-22 g, 4-6 weeks, tail vein injected with C. neoformans H99 cells)[1]
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Dosage:15 mg/kg
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Administration:Intragastrically, daily for 5 days
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Result:Showed potent anti-Cryptococcal efficacy, significantly reduced the number of C. neoformans H99 cells in the brain after 5 days, prolong the median survival time (14 days) of the infected mice at a dose of 15 mg/kg.
Chemical Information
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CAS. Nr. 2640054-39-1
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Molecular Weight 446.86
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Formel C21H26Cl3NOS
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SMILES
ClC1=CC(C2C3=C(C(CC2)NCCC4CCOCC4)C=CS3)=CC=C1Cl.[H]Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Antifungal agent 22 Related Classifications
HY-144632 Related Classifications
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