| Description | Lamivudine (BCH-189) is a reverse transcriptase inhibitor and ZALCITABINE analog in which a sulfur atom replaces the 3' carbon of the pentose ring. It is used to treat HIV disease. |
| In vivo | Lamivudine具有特异的抗脱氧胞苷激酶的活性,HBV聚合酶的非天然的L-构型的dNTP的不寻常的底物,而PCV的抗HBV活性归因于脱氧胞苷激酶的非常宽的底物特异性和HBV聚合酶对非天然L-构象的dNTPs的不寻常底物偏好,而PCV的抗-HBV活性似乎取决于若干因素,包括最佳磷酸化（足够对于抗病毒活性而不是细胞毒性）,PCV-TP的长细胞内半衰期和PCV-TP抑制HBV RT引发反应以及RT和DNA聚合酶活性的能力。Lamivudine和喷昔洛韦抑制鸭乙型肝炎病毒的复制,其联合使用时,两种核苷类似物在各种临床相关浓度下协同作用。Lamivudine和喷昔洛韦联用比单独两种药物更有效地减少DHBV的常顽固病毒共价闭合环状（CCC）DNA的形式。Lamivudine在PBMC 中,抑制HIV-I产生的p24抗原产量,ED50s范围为0.07 μM到0.2 μM。 |
| Synonyms | GR109714X, BCH-189, 拉米夫定 |
| molecular weight | 229.26 |
| Molecular formula | C8H11N3O3S |
| CAS | 134678-17-4 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/mL (239.9 mM) Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: 42 mg/mL (183.2 mM) |
| References | 1. Shaw T, et al. J Viral Hepat, 1999, 6(2), 89-106. 2. Colledge D, et al. Hepatology, 1997, 26(1), 216-225. 3. Merrill DP, et al. J Infect Dis, 1996, 173(2), 355-364. 4. Wu Y, Yang J, Duan C, et al. Simultaneous determination of antiretroviral drugs in human hair with liquid chromatography-electrospray ionization-tandem mass spectrometry[J]. Journal of Chromatography B. 2018 Apr 15;1083:209-221. 5. Herrmann A, Roesner M, Werner T, et al. Potent inhibition of HIV replication in primary human cells by novel synthetic polyketides inspired by Aureothin[J]. Scientific Reports. 2020, 10(1): 1-15. 6. Xie B, Sun D, Du Y, et al. A two-step lineage reprogramming strategy to generate functionally competent human hepatocytes from fibroblasts[J]. Cell research. 2019: 1. |
| Citations | 1. Xie B, Sun D, Du Y, et al. A two-step lineage reprogramming strategy to generate functionally competent human hepatocytes from fibroblasts. Cell research. 2019: 1. 2. Herrmann A, Roesner M, Werner T, et al. Potent inhibition of HIV replication in primary human cells by novel synthetic polyketides inspired by Aureothin. Scientific Reports. 2020, 10(1): 1-15 3. Wu Y, Yang J, Duan C, et al. Simultaneous determination of antiretroviral drugs in human hair with liquid chromatography-electrospray ionization-tandem mass spectrometry. Journal of Chromatography B. 2018 Apr 15;1083:209-221 4. Bao H, Yan J, Huang J, et al.Activation of endogenous retrovirus triggers microglial immuno-inflammation and contributes to negative emotional behaviors in mice with chronic stress.Journal of Neuroinflammation.2023, 20(1): 1-16. |