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ChemicalBook--->CAS DataBase List--->1001670-19-4

1001670-19-4

1001670-19-4 Structure

1001670-19-4 Structure
IdentificationBack Directory
[Name]

L-Valine, ester with 2',3'-dideoxy-3'-fluoroguanosine 5'-[(2S)-2-hydroxypropanoate]
[CAS]

1001670-19-4
[Synonyms]

Lagociclovir valactate
L-Valine, ester with 2',3'-dideoxy-3'-fluoroguanosine 5'-[(2S)-2-hydroxypropanoate]
[Molecular Formula]

C18H25FN6O6
[MOL File]

1001670-19-4.mol
[Molecular Weight]

440.43
Chemical PropertiesBack Directory
[Boiling point ]

679.8±65.0 °C(Predicted)
[density ]

1.65±0.1 g/cm3(Predicted)
[pka]

7.58±0.33(Predicted)
Hazard InformationBack Directory
[Uses]

Lagociclovir valactate is a prodrug of Lagociclovir (HY-14844). Lagociclovir valactate is an orally active anti-HBV agent[1].
[in vivo]

Lagociclovir valactate (20 or 60 mg/kg; p.o.; daily for 10 weeks) shows anti-woodchuck hepatitis virus (WHV) activity in woodchucks[1].

Animal Model:Woodchucks with chronic WHV infection[1]
Dosage:20 or 60 mg/kg
Administration:Oral, daily for 10 weeks
Result:Reduced WHV viremia effectively and maintained WHV DNA at a very low level.
Animal Model:Woodchucks[1]
Dosage:10 or 40 mg/kg
Administration:Oral (Pharmacokinetic Analysis)
Result:Average pharmacokinetic parameters for Lagociclovir after oral administration of Lagociclovir valactate to healthy and chronically WHV infected woodchucks[1]
Pharmacokinetic parameter for LagociclovirHealthy woodchucks (n = 4) receiving Lagociclovir valactate at 10 mg/kgHealthy woodchucks (n = 4) receiving Lagociclovir valactate at 40 mg/kgWHV-infected woodchucks (n = 14) receiving Lagociclovir valactate at 60 mg/kg
Cmax (μM)0.54 ± 0.142.10 ± 1.53.50 ± 1.9
Tmax (h)4.10 ± 1.03.30 ± 1.52.90 ± 1.1
AUC0-∞ (μM ? h/liter)5.15 ± 1.010.50 ± 4.220.1 ± 11.3
t1/2 (h)5.44 ± 1.24.20 ± 1.64.7 ± 0.8
[References]

[1] Michalak TI, et al. Profound antiviral effect of oral administration of MIV-210 on chronic hepadnaviral infection in a woodchuck model of hepatitis B. Antimicrob Agents Chemother. 2009 Sep;53(9):3803-14. DOI:10.1128/AAC.00263-09
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