Amphihevir
Amphihevir is an orally active HCV NS4B inhibitor. Amphihevir exhibits activity against HCV genotype 1a and 1b replicons and reduces HCV RNA levels. Amphihevir can be used in the research of chronic hepatitis C.
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- CAS. Nr.: 1890171-61-5
- Formel: C21H19F3N4O4
- Molecular Weight:448.40
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Help & FAQs
Biologische Aktivität
Beschreibung
In Vitro
Amphihevir potently inhibits HCV GT1a (H77) replicon cells with an EC50 of 0.34 nM; it inhibits HCV GT1b (Con1) replicon cells with EC50 values of 1.97 nM (luciferase assay) and 1.12 nM (qRT-PCR assay), respectively; it also moderately inhibits HCV GT2a (JFH-1) HCVcc with an EC50 of 186 nM; and its antiviral activity decreases as the concentration of human serum increases[1].
Amphihevir (12-300 nM; 9 h) inhibits RNA replication in HCV GT1b (Con1) replicon-stable cells[1].
Amphihevir exhibits additive to highly synergistic anti-HCV activity with other direct-acting antiviral agents in HCV GT1b (Con1) replicon cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCV genotype 1b (Con1) replicon stable cells
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Concentration:12 nM, 60 nM, 300 nM
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Incubation Time:9 h
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Result:Caused a continuous, concentration-dependent decline in HCV-1b replicon RNA over 9 days, with no RNA rebound observed.
Reduced replicon RNA by nearly 6,300-fold (3.8 Log10) at 300 nM (25× EC90).
Parmacokinetics
| Species | Dose | Route | C0 | T1/2 | Vdss | CL | AUC0-last | AUC0-inf | Cmax | Tmax | MRT0-last | MRT0-inf | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 673 ng/mL | 1.15 h | 1.67 L/kg | 17.8 mL/min/kg | 959 ng·h/mL | 965 ng·h/mL | / | / | / | / | / |
| Rat[1] | 3 mg/kg | p.o. | / | 2.74 h | / | / | 1610 ng·h/mL | 1630 ng·h/mL | 311 ng/mL | 2.00 h | / | / | 65.1 % |
| Rat[1] | 10 mg/kg | p.o. | / | 4.16 h | / | / | 3820 ng·h/mL | 3900 ng·h/mL | 507 ng/mL | 1.50 h | / | / | 40.1 % |
| Rat[1] | 10 mg/kg | p.o. | / | 4.7 h | / | / | 3205 ng·h/mL | 3510 ng·h/mL | 345 ng/mL | 3.84 h | / | / | / |
| Rat[1] | 30 mg/kg | p.o. | / | 8.98 h | / | / | 10600 ng·h/mL | 12700 ng·h/mL | 899 ng/mL | 2.67 h | / | / | 43.1 % |
| Dog[1] | 1 mg/kg | i.v. | 555 ng/mL | 4.45 h | 2.30 L/kg | 9.30 mL/min/kg | 1880 ng·h/mL | 1930 ng·h/mL | / | / | / | / | / |
| Dog[1] | 3 mg/kg | p.o. | / | 4.38 h | / | / | 758 ng·h/mL | 787 ng·h/mL | 145 ng/mL | 1.25 h | 5.33 h | 6.18 h | 13.8 % |
| Dog[1] | 10 mg/kg | p.o. | / | 4.72 h | / | / | 3520 ng·h/mL | 4260 ng·h/mL | 438 ng/mL | 1.50 h | 7.61 h | 10.7 h | 18.5 % |
| Dog[1] | 10 mg/kg | p.o. | / | 4.51 h | / | / | 2560 ng·h/mL | 2880 ng·h/mL | 371 ng/mL | 1.50 h | 7.19 h | 9.27 h | 13.3 % |
| Dog[1] | 30 mg/kg | p.o. | / | 11.3 h | / | / | 7150 ng·h/mL | 10400 ng·h/mL | 681 ng/mL | 1.33 h | 8.17 h | 16.8 h | 12.6 % |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (SD) rats (male and female)[1]
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Dosage:1; 3; 10 ; 20 ; 60 ; 200 mg/kg
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Administration:i.v.; single dose; p.o.; single dose; p.o.; daily; 7 days; p.o.; daily; 4 weeks
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Result:Exhibited moderate to favorable oral absorption.
Chemical Information
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CAS. Nr. 1890171-61-5
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Molecular Weight 448.40
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Formel C21H19F3N4O4
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SMILES
N#CC1=C(C(N2CCN(CC2)N3C(OCC3)=O)=O)OC4=C1C=C(C5CC5)C=C4C(F)(F)F
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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)
Amphihevir Related Classifications
HY-182691 Related Classifications
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