产品
编 号：F130425
分子式：C8H11N3O3S
分子量：229.26
分子式：C8H11N3O3S
分子量：229.26
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
100mg
624
In-stock
500mg
1584
In-stock
结构图
CAS No: 134678-17-4
产品详情
生物活性：
Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS.
体内研究：
Lamivudine (20-500 mg/kg/d; p.o.; 15 or 45 d) causes oxidative stress and is toxic to rat liver.Lamivudine (50 mg/kg; i.p.; single dose) penetrates well in CNS and localizes in brain regions susceptible to HIV neurodegeneration in rat. Pharmacokinetic Parameters of Lamivudine in HIV-infected RatsParameterCmax (μg/mL)Tmax (h)T1/2 (h)AUC (h·ng/mL)
Plasma25,8460.250.6822,172
Brain2720.51.2967
Pharmacokinetic data measured over a 24-h period, sampling was done at 0.25, 0.5, 1.0, 2.0, 4.0, 6.0, 8.0, and 24.0 h postdose.Animal Model:Wistar female rats
Dosage:20-500 mg/kg/day
Administration:Oral gavage; single or repeated dose; 15 or 45 days
Result:Increased activities of the aminotransferases (ALT and AST), γ-glutamyltransferase (GGT) and total protein concentration in serum at 500 mg/kg dose.Increased activities of glutathione S-transferase (GST), GGT and superoxide dismutase (SOD) as well as concentrations of malondialdehyde (MDA) and protein at 20 mg/kg dose.Caused multifocal lymphocyte population and hepatocyte edema degeneration in hepatic sinusoids of chickens.
体外研究：
Lamivudine (1 μM) is potent inhibitor of hepatitis B virus (HBV) replication, shows antiviral activity in primary duck hepatocyte (PDH) cultures derived from ducklings congenitally infected with the duck hepatitis B virus (DHBV).Lamivudine (0-20 μM; 2, 4, 9 d) inhibits DHBV replication with 50% inhibitory concentration of 0.55 μM.Lamivudine, combinded with penciclovir (9-[2-hydroxy-1-(hydroxymethyl)ethoxymethyl]guanine [PCV]), (1 μM; 2, 4, 9 d) shows synergistic effect, acts potent function in reducing the normally recalcitrant viral covalently closed circular (CCC) DNA form of DHBV.
Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS.
体内研究：
Lamivudine (20-500 mg/kg/d; p.o.; 15 or 45 d) causes oxidative stress and is toxic to rat liver.Lamivudine (50 mg/kg; i.p.; single dose) penetrates well in CNS and localizes in brain regions susceptible to HIV neurodegeneration in rat. Pharmacokinetic Parameters of Lamivudine in HIV-infected RatsParameterCmax (μg/mL)Tmax (h)T1/2 (h)AUC (h·ng/mL)
Plasma25,8460.250.6822,172
Brain2720.51.2967
Pharmacokinetic data measured over a 24-h period, sampling was done at 0.25, 0.5, 1.0, 2.0, 4.0, 6.0, 8.0, and 24.0 h postdose.Animal Model:Wistar female rats
Dosage:20-500 mg/kg/day
Administration:Oral gavage; single or repeated dose; 15 or 45 days
Result:Increased activities of the aminotransferases (ALT and AST), γ-glutamyltransferase (GGT) and total protein concentration in serum at 500 mg/kg dose.Increased activities of glutathione S-transferase (GST), GGT and superoxide dismutase (SOD) as well as concentrations of malondialdehyde (MDA) and protein at 20 mg/kg dose.Caused multifocal lymphocyte population and hepatocyte edema degeneration in hepatic sinusoids of chickens.
体外研究：
Lamivudine (1 μM) is potent inhibitor of hepatitis B virus (HBV) replication, shows antiviral activity in primary duck hepatocyte (PDH) cultures derived from ducklings congenitally infected with the duck hepatitis B virus (DHBV).Lamivudine (0-20 μM; 2, 4, 9 d) inhibits DHBV replication with 50% inhibitory concentration of 0.55 μM.Lamivudine, combinded with penciclovir (9-[2-hydroxy-1-(hydroxymethyl)ethoxymethyl]guanine [PCV]), (1 μM; 2, 4, 9 d) shows synergistic effect, acts potent function in reducing the normally recalcitrant viral covalently closed circular (CCC) DNA form of DHBV.
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