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Lamivudine

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Chemical Structure| 134678-17-4 同义名 : 拉米呋啶 ;BCH-189;3TC;Lamivudine, 3TC, Epivir, Zeffix, Heptovir, BCH-189;2’,3’-dideoxy-3’-Thiacytidine;(-)-BCH 189;GR109714X
CAS号 : 134678-17-4
货号 : A107352
分子式 : C8H11N3O3S
纯度 : 98%
分子量 : 229.256
MDL号 : MFCD00869739
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(218.1 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(218.1 mM)
动物实验配方：
生物活性
描述 Lamivudine is a cytidine analog that inhibits HIV-1 reverse transcriptase with an IC50 value of 0.045μM.[4] In human HBV-transfected cell line HepG2 2.2.15, the combined treatment of lamivudine (30μg/mL) and matrine at 100, 200, or 400 μg/mL for 9 days significantly inhibited the secretion of HBeAg into culture media (63%, 68%, and 75%, respectively). The solo use of lamivudine (30μg/mL) or in combination with matrine also significantly decreased the intracellular hepatitis B virus (HBV)-DNA level. The intracellular HBV-DNA inhibition rate of lamivudine (30μg/mL) was 79%.[5] Daily exposure of HBV transgenic mice to lamivudine (100mg/kd/d) from day 5 or day 10 of gestation resulted in a significant decrease in the level of HBV DNA, without affecting the postnatal survival of live pups.[3]
作用机制 Lamivudine is a potent antiviral nucleotide analog that inhibits the reverse transcriptases of both HIV and HBV.[3]
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
2.2.15 cells Function assay Antiviral activity against Hepatitis B virus (HBV) in 2.2.15 cells, EC50=0.008 μM 11052795
CEM-SS cells Function assay Antiviral activity against HIV-1 subtype 3B infected in CEM-SS cells assessed as inhibition of viral replication after 6 days by XTT assay, EC50=0.2 μM 22858097
HEK293 cells Function assay 72 h Antiviral activity against HIV1 subtype D isolate 8 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=3.25 μM 20308377
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00158821 HIV Infections Phase 3 Completed - -
NCT00226447 Chronic Hepatitis B Phase 2 Completed - China ... 展开 >> Cheng Suen Man Shook Hepatitis Center, Institute of Digestive Disease, The Chinese University of Hong Kong, Prince of Wales Hospital Hong Kong SAR, China 收起 <<
NCT01844297 AIDS/HIV PROBLEM Not Applicable Unknown December 2015 China, Beijing ... 展开 >> Peking Union Medical College Hospital Not yet recruiting Beijing, Beijing, China, 100730 Contact: Wei Lv, MD    86-10-69155082    lvweipumch@163.com    Principal Investigator: Taisheng Li, MD 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.36mL

0.87mL

0.44mL

21.81mL

4.36mL

2.18mL

43.62mL

8.72mL

4.36mL
参考文献

[1]Shaw T, Locarnini SA. Preclinical aspects of lamivudine and famciclovir against hepatitis B virus. J Viral Hepat. 1999 Mar;6(2):89-106.

[2]Colledge D, Locarnini S, Shaw T. Synergistic inhibition of hepadnaviral replication by lamivudine in combination with penciclovir in vitro. Hepatology. 1997 Jul;26(1):216-25.

[3]Li D, Xu DZ, Choi BC, Men K, Zhang JX, Lei XY, Yan YP. Preliminary study on the efficacy and safety of lamivudine and interferon alpha therapy in decreasing serum HBV DNA level in HBV positive transgenic mice during pregnancy. J Med Virol. 2005 Jun;76(2):203-7

[4]Perez-Olmeda M, Garcia-Perez J, Mateos E, Spijkers S, Ayerbe MC, Carcas A, Alcami J. In vitro analysis of synergism and antagonism of different nucleoside/nucleotide analogue combinations on the inhibition of human immunodeficiency virus type 1 replication. J Med Virol. 2009 Feb;81(2):211-6

[5]Ma ZJ, Li Q, Wang JB, Zhao YL, Zhong YW, Bai YF, Wang RL, Li JY, Yang HY, Zeng LN, Pu SB, Liu FF, Xiao DK, Xia XH, Xiao XH. Combining Oxymatrine or Matrine with Lamivudine Increased Its Antireplication Effect against the Hepatitis B Virus In Vitro. Evid Based Complement Alternat Med. 2013;2013:186573