CZx-243
CZx-243 is an orally active broad-spectrum antifungal agent. CZx-243 binds to the active site of fungal CYP51 and interferes with ergosterol biosynthesis by depleting ergosterol and causing the accumulation of upstream sterol intermediates. CZx-243 blocks yeast-to-hypha transition; it inhibits the membrane integrity of fungi such as Candida glabrata and Cryptococcus neoformans. CZx-243 significantly reduces renal fungal burden in a systemic mouse model of invasive fungal infection resistant to Fluconazole (HY-B0101). CZx-243 can be used in the research of fungal infections.
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- Formule: C27H21ClF2N4O2
- Masse moléculaire:506.93
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Stockage:
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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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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CYP51 |
CZx-243 (compound D27) potently inhibits the growth of susceptible fungal species including C. albicans (SC5314), C. albicans (CPCC400616), C. tropicalis (GIM 2.183), C. parapsilosis (GIM 2.190), C. glabrata (clinical isolation), C. krusei (AS 2.1045), C. neoformans (CGMCC 2.3161), and A. fumigatus (CGMCC 3.7795) with MIC values ranging from 0.00625 to 0.125 μg/mL[1].
CZx-243 potently inhibits the growth of Fluconazole (HY-B0101)-resistant C. albicans Strain 17# with an MIC80 of 0.0625 μg/mL[1].
CZx-243 disrupts cell membrane integrity and causes morphological damage to C. albicans (ATCC SC5314) cells after 48 h of incubation at 35 °C[1].
CZx-243 potently inhibits biofilm formation in C. glabrata (clinical isolation) and C. neoformans (CGMCC 2.3161) with SMIC50 values of 0.0625 μg/mL and 0.5 μg/mL respectively[1].
CZx-243 (2-8 μg/mL) suppresses the yeast-to-hyphae morphological transition in C. albicans (CPCC400616)[1].
CZx-243 (0.05 μg/mL; 16 h) inhibits ergosterol biosynthesis in C. albicans (SC5314) and C. neoformans (CGMCC 2.3161), causing profound depletion of ergosterol and accumulation of upstream sterol intermediates[1].
CZx-243 exhibits moderate inhibition of human CYP1A2, CYP2C9, CYP2C19, and CYP3A4 enzymes with IC50 values ranging from 3.74 to 9.82 μM[1].
CZx-243 has low cytotoxicity against HUVEC and SH-SY5Y cells, with IC50 values of 16.24 μM and 25.75 μM respectively, and high selectivity for fungal cells over human cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
CZx-243 (500 mg/kg; p.o.; single dose; 7 days) is well-tolerated in ICR mice, with 100% survival, no significant weight change, and no observable histopathological damage to liver or kidney tissues over 7 days[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice (4-6 weeks old, specific pathogen-free, immunosuppressed with intraperitoneal cyclophosphamide)[1]
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Dosage:5 mg/kg; 10 mg/kg
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Administration:p.o.; daily; 5 days
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Result:Reduced average renal fungal load to 2.67 × 103 CFU/mL (log10 3.3465) at 5 mg/kg.
Reduced average renal fungal load to 1.58 × 103 CFU/mL (log10 3.1590) at 10 mg/kg.
Produced statistically significant reduction in fungal load.
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Animal Model:ICR mice (6-8 weeks old, specific pathogen-free, male and female, 20-25 g)[1]
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Dosage:500 mg/kg
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Administration:p.o.; single dose; 7 days
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Result:Achieved 100% survival rate of treated mice over 7 days.
Showed no significant difference in body weight between treatment group and control group.
Revealed no significant structural changes in liver and kidney tissues.
Chemical Information
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Masse moléculaire 506.93
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Formule C27H21ClF2N4O2
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SMILES
FC1=C([C@](O)([C@H](N2C=CC(C=C(C=C3)C4=CC=C(C=C4)Cl)=C3C2=O)C)CN5C=NC=N5)C=CC(F)=C1
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CZx-243 Related Classifications
HY-187376 Related Classifications
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