Lamivudine

立即咨询

Lamivudine

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

134678-17-4

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	电议
10mg	电议
50mg	电议

产品介绍

化学性质

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	229.26
Cas No.	134678-17-4
Formula	C₈H₁₁N₃O₃S
Solubility	≥10.5 mg/mL in DMSO; ≥11.4 mg/mL in EtOH with ultrasonic; ≥89.4 mg/mL in H2O with ultrasonic
Chemical Name	4-amino-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2-one
Canonical SMILES	C1C(OC(S1)CO)N2C=CC(=NC2=O)N
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

Lamivudine, a nucleoside analog, is a potent reverse transcriptase inhibitor, with IC50 value of 0.316 μM against human immunodeficiency virus type 1 (HIV-1) [1].

Reverse transcriptase is a RNA-dependent DNA polymerase, playing a critical role in retroviral replication. Thus, reverse transcriptase has been made a target of antiretroviral chemotherapy [1].

Lamivudine was most potent against simian retrovirus types 1 and 2 (SRV-1, SRV-2), and HIV-1, with IC50 values of 10, 0.316 and 0.316 μM, respectively, but did not inhibit foamy viruses and amphotrophic murine leukaemia virus (MLV-A) [1].

In human coinfected with HIV-1 and hepatitis B virus (HBV), Lamivudine (150 mg, b.i.d., p.o.) displayed dual efficacy through both delayed HIV-1 disease progression and a favorable biochemical and HBV virologic response. Twelve months of Lamivudine therapy led to HBV DNA and hepatitis B e antigen (HBeAg) losses of ~40% and ~20%, respectively, and more alanine aminotransferase (ALT) normalization than that in the placebo group [2].

References:

[1]. Rosenblum L L, Patton G, Grigg A R, et al. Differential susceptibility of retroviruses to nucleoside analogues. Antiviral Chemistry and Chemotherapy, 2001, 12(2): 91-97.

[2]. Dore G J, Cooper D A, Barrett C, et al. Dual efficacy of lamivudine treatment in human immunodeficiency virus/hepatitis B virus-coinfected persons in a randomized, controlled study (CAESAR). The CAESAR Coordinating Committee. The Journal of Infectious Diseases, 1999, 180(3): 607-613.

试验操作

Cell experiment:[1]
Cell lines	Peripheral blood mononuclear cells (PBMCs)
Reaction Conditions	10 d incubation
Applications	Lamivudine inhibited p24 antigen production by HIV-I in PBMCs, with ED50s ranging from 0.07 to 0.2 μM. There was no toxicity in uninfected PBMC with concentrations of lamivudine up to 10 μM over a 10-day culture period.
Animal experiment:[2]
Animal models	Humanized BALB/c Rag1^-/-γc^-/-or Rag2^-/-γc^-/-mice
Dosage form	7 mg drug tablet containing lamivudine, abacavir and dolutegravir Re-suspended in 100 μl distilled water for daily gavage
Applications	Oral drug treatment led to full viral suppression and protection from CD4 T cell depletion. Cessation of therapy resulted in viral rebound and CD4 T cell loss.
Note	The technical data provided above is for reference only.
	References: 1. Merrill DP, Moonis M, Chou TC, et al. Lamivudine or stavudine in two- and three-drug combinations against human immunodeficiency virus type 1 replication in vitro. The Journal of Infectious Diseases, 1996, 173(2): 355-364. 2. Hu S, Neff CP, Kumar DM, et al. A humanized mouse model for HIV-2 infection and efficacy testing of a single-pill triple-drug combination anti-retroviral therapy. Virology, 2017, 501: 115-118.