Lamivudine (BCH-189) 是一种具有口服活性的核苷逆转录酶 (nucleoside reverse transcriptase) 抑制剂 (NRTI)。Lamivudine 可以抑制HIV逆转录酶 1 和 2 以及乙型肝炎病毒 (hepatitis B virus) 的逆转录酶。Lamivudine 可以透过血脑屏障。
| 生物活性 | Lamivudine (BCH-189) is an orally activenucleosidereverse transcriptaseinhibitor (NRTI). Lamivudine can inhibitHIVreverse transcriptase1/2and also thereverse transcriptaseofhepatitis B virus. Lamivudine salicylate can penetrate the CNS[1][2]. |
体外研究
(In Vitro) | 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)[1].
Lamivudine (0-20 μM; 2, 4, 9 d) inhibits DHBV replication with 50% inhibitory concentration of 0.55 μM[1].
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[1].
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体内研究
(In Vivo) | Lamivudine (20-500 mg/kg/d; p.o.; 15 or 45 d) causes oxidative stress and is toxic to rat liver[2].
Lamivudine (50 mg/kg; i.p.; single dose) penetrates well in CNS and localizes in brain regions susceptible to HIV neurodegeneration in rat[3].
Pharmacokinetic Parameters of Lamivudine in HIV-infected Rats[3]
| Parameter | Cmax(μg/mL) | Tmax(h) | T1/2(h) | AUC (h·ng/mL) | | Plasma | 25,846 | 0.25 | 0.68 | 22,172 | | Brain | 272 | 0.5 | 1.2 | 967 |
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[2] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: H2O : ≥ 50 mg/mL(218.09 mM) DMSO : 50 mg/mL(218.09 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 4.3619 mL | 21.8093 mL | 43.6186 mL | | 5 mM | 0.8724 mL | 4.3619 mL | 8.7237 mL | | 10 mM | 0.4362 mL | 2.1809 mL | 4.3619 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 100 mg/mL (436.19 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (10.90 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (10.90 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (10.90 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (10.90 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 4. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (10.90 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (10.90 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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