Antifungal agent 151
Antifungal agent 151 is a Prp8 intein inhibitor that inhibits the self-splicing process of the Prp8 intein, preventing maturation of the Prp8 protein. Antifungal agent 151 exerts in vitro antifungal activity against Cryptococcus neoformans and Cryptococcus gattii. Antifungal agent 151 can be used for the research of cryptococcus pneumonia.
For research use only. We do not sell to patients.
- CAS No.: 3097563-43-1
- Formula: C16H12FN3O3S2
- Molecular Weight:377.41
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Antifungal agent 151 (compound B5) (1-64 μg/mL; 48 h) potently inhibits the growth of C. neoformans H99, C. gattii R265, fluconazole-resistant C. neoformans (strain 313), and clinical isolates of C. neoformans with MIC values ranging from 0.5 to 2 μg/mL[1].
Antifungal agent 151 (compound B5) (8.0 μg/mL; until fungal elimination) exhibits rapid, concentration-dependent fungicidal activity against C. neoformans H99, eliminating the fungus within two hours[1].
Antifungal agent 151 (compound B5) (2.0 μg/mL; 2 h) induces transcriptomic remodeling and inhibits proper intron splicing in C. neoformans H99, leading to oxidative stress, DNA damage responses, and altered metabolic gene expression[1].
Antifungal agent 151 (compound B5) binds to the Prp8 intein active site via hydrogen bonds and a favorable distance for covalent interaction with Cys1[1].
Antifungal agent 151 (compound B5) has IC50 values of 14.99 μg/mL against LO2 cells and 10.31 μg/mL against A549 cells. Antifungal agent 151shows a lower MIC value against C. neoformans, conferring a higher therapeutic index than 6G-318S[1].
Antifungal agent 151 (compound B5) (64 μg/mL) shows good blood compatibility with a 3.2% hemolysis rate at 64 μg/mL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 6-8 weeks old, intranasally inoculated with C. neoformans H99)[1]
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Dosage:10 mg/kg
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Administration:i.p.; daily; 7 days
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Result:Significantly reduced pulmonary fungal burden; suppressed fungal invasion in lung tissues; reduced focal lymphocyte infiltration; preserved alveolar structural integrity compared to saline-treated controls.
Chemical Information
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CAS No. 3097563-43-1
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Molecular Weight 377.41
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Formula C16H12FN3O3S2
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SMILES
FC1=CC=C(NC(C2=C(S(C3=CC=C(C)C=C3)(=O)=O)SN=N2)=O)C=C1
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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)