Antifungal agent-166
Antifungal agent-166 is an antifungal agent. The combination of Antifungal agent-166 and Fluconazole exerts synergistic bacteriostatic effects against fluconazole-resistant Candida albicans. Antifungal agent-166 exhibits bacteriostatic activity against both Candida glabrata and Cryptococcus neoformans. Antifungal agent-166 reverses the fluconazole resistance of strains by downregulating ergosterol synthesis-related genes, drug resistance-related genes and virulence-related genes. Antifungal agent-166 can enhance the efficacy of Fluconazole in Galleria mellonella and mouse candidiasis models, reduce fungal load and improve survival rate. Antifungal agent-166 can be used in the research of fungal infections.
For research use only. We do not sell to patients.
- CAS No.: 3122934-62-4
- Formula: C24H21F2N9O2S
- Molecular Weight:537.54
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Antifungal agent-166 (Compound A21) (48 h), in combination with Fluconazole (HY-B0101), exhibits strong synergistic antifungal activity against fluconazole-tolerant Candida albicans strains 938 and 939; it reduces the MIC of fluconazole to ≤0.125 μg/mL, with an FICI of 0.127[1].
Antifungal agent-166 (48-72 h) potently inhibits Candida glabrata 537 (MIC = 1.0 μg/mL) and moderately inhibits Cryptococcus neoformans 32609 (MIC = 4.0 μg/mL)[1].
Antifungal agent-166 (0.5 μg/mL; 8 h) enhances the inhibitory effect of Fluconazole on ergosterol biosynthesis in Fluconazole-resistant Candida albicans 939; when used in combination with Fluconazole, it eliminates detectable ergosterol and increases the accumulation of bypass pathway sterols[1].
Antifungal agent-166 (8 μg/mL; 24 h) exhibits moderate cytotoxicity against HUVEC, with an IC50 value of 16.41 μg/mL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human umbilical vein endothelial cells (HUVECs)
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Concentration:8 μg/mL (alone); 8 μg/mL (combined with 8 μg/mL fluconazole)
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Incubation Time:24 h
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Result:Resulted in 63.99% cell viability with an IC50 of 16.41 μg/mL when used alone.
Resulted in 58.72% cell viability with an IC50 of 14.42 μg/mL when combined with Fluconazole.
Had a selectivity index (IC50/MIC) exceeding 110, based on its effective synergistic antifungal concentration of ≤0.125 μg/mL.
Antifungal agent-166 (0.5 mg/kg; topical administration; single dose), in combination with Fluconazole significantly reduces cutaneous fungal burden in a mouse model of cutaneous candidiasis[1].
Antifungal agent-166 (0.25-0.5 mg/kg, i.p.; once daily; for 3 consecutive days), in combination with Fluconazole dose-dependently reduces renal fungal burden in a mouse model of systemic candidiasis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:larvae (weight ~500 mg)[1]
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Dosage:0.5 mg/kg (monotherapy); 0.5 mg/kg (in combination with Fluconazole 1 mg/kg)
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Administration:injection; single dose
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Result:Resulted in a median larval survival time of 2 days and a final survival rate of 33%.
Prolonged median survival time and reached a final survival rate of 73%, representing a 40% increase compared to fluconazole alone.
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Animal Model:C57BL/6 (female, 4-6 weeks old, 18-22 g, immunosuppressed with daily intraperitoneal dexamethasone 25 mg/kg for 3 days)[1]
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Dosage:0.5 mg/kg (monotherapy); 0.5 mg/kg (in combination with Fluconazole 1 mg/kg)
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Administration:topical; single dose
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Result:Did not reduce skin fungal burden compared to the control.
Reduced the skin fungal burden from a Log10 CFU/cm2 value of 3.28 to 1.86 when administered in combination with fluconazole.
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Animal Model:ICR (female, 4-6 weeks old, 18-22 g)[1]
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Dosage:0.5 mg/kg (monotherapy); 0.25 mg/kg (in combination with Fluconazole 0.25 mg/kg); 0.5 mg/kg (in combination with Fluconazole 0.25 mg/kg)
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Administration:i.p.; daily; 3 days
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Result:Did not reduce kidney fungal burden compared to the control.
Reduced the kidney fungal burden from a Log10 CFU/g value of 6.58 to 4.99 when administered at 0.25 mg/kg in combination with fluconazole 0.25 mg/kg.
Reduced the kidney fungal burden from a Log10 CFU/g value of 6.58 to 4.28 when administered at 0.5 mg/kg in combination with fluconazole 0.25 mg/kg.
Showed reduced fungal colonization and hyphal formation in kidney tissue from mice receiving the combination treatment compared to control or monotherapy groups.
Chemical Information
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CAS No. 3122934-62-4
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Molecular Weight 537.54
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Formula C24H21F2N9O2S
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SMILES
S=C(NNC1=NC(NCC2=CC=C(F)C=C2)=NC(NCC3=CC=C(F)C=C3)=N1)NC4=CC=C([N+]([O-])=O)C=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Antifungal agent-166 Related Classifications
HY-184314 Related Classifications
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