2. Anti-infection
  3. HCV
  4. 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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Amphihevir

Amphihevir Chemical Structure

CAS No. : 1890171-61-5

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Amphihevir Related Antibodies

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Description

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[1].

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.

Amphihevir Related Antibodies

Real Time qPCR[1]

Cell Line: HCV genotype 1b (Con1) replicon stable cells
Concentration: 12 nM, 60 nM, 300 nM
Incubation Time: 9 h
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

Amphihevir (1-200 mg/kg; i.v.; p.o.; single/daily administration; 1-4 weeks) exhibits moderate to favorable oral absorption in SD rats and Beagle dogs, with no obvious drug accumulation following repeated administration[1].

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

Animal Model: Sprague-Dawley (SD) rats (male and female)[1]
Dosage: 1; 3; 10 ; 20 ; 60 ; 200 mg/kg
Administration: i.v.; single dose; p.o.; single dose; p.o.; daily; 7 days; p.o.; daily; 4 weeks
Result: Exhibited moderate to favorable oral absorption.
Molecular Weight

448.40

Formula

C21H19F3N4O4
CAS No.
SMILES

N#CC1=C(C(N2CCN(CC2)N3C(OCC3)=O)=O)OC4=C1C=C(C5CC5)C=C4C(F)(F)F
Shipping

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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Amphihevir Related Classifications

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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.

Keywords:

Amphihevir1890171-61-5HCVHepatitis C virushuman-derived cell linesNS5B inhibitorsHepatitis C virus NS4BBeagle dogsSD ratsNS5A inhibitorsHepatitis C viral RNAHepatitis C virus genotype 1aHepatitis C virus genotype 1bNS3/4A inhibitorsInhibitorinhibitorinhibit

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