1. Anti-infection
  2. Fungal
  3. 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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Antifungal agent 22 Chemical Structure

Antifungal agent 22 Chemical Structure

CAS No. : 2640054-39-1

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Description

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[1].

IC50 & Target

IC50: 0.5 μg/mL (Fungal)[1].

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.

Cell Proliferation Assay

Cell Line: C. neoformans H99 cells[1]
Concentration: 0, 1, 2, 4, 8 μg/mL
Incubation Time: 0, 4, 8, 12, 24, 48, and 72 h
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.

Cell Viability Assay

Cell Line: Fungal cells (RPMI 1640 medium)[1]
Concentration: 0, 0.5, 1, 2, 4, 8 μg/mL
Incubation Time: 48, 72 h
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

Antifungal agent 22 (D16) (15 mg/kg, Intragastrically, daily for 5 days) shows potent anti-Cryptococcal efficacy[1].

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

Animal Model: ICR female mice (18-22 g, 4-6 weeks, tail vein injected with C. neoformans H99 cells)[1]
Dosage: 15 mg/kg
Administration: Intragastrically, daily for 5 days
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.
Molecular Weight

446.86

Formula

C21H26Cl3NOS

CAS No.
SMILES

ClC1=CC(C2C3=C(C(CC2)NCCC4CCOCC4)C=CS3)=CC=C1Cl.[H]Cl

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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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Antifungal agent 22 Related Classifications

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  • Do most proteins show cross-species activity?

    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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Antifungal agent 22
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