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Lamivudine

Catalog No.
A8458
Nucleoside analog reverse transcriptase inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$80.00
In stock
10mg
$45.00
In stock
50mg
$130.00
In stock

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Email: [email protected]

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Background

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt229.26
Cas No.134678-17-4
FormulaC8H11N3O3S
Solubility≥10.5 mg/mL in DMSO; ≥11.4 mg/mL in EtOH with ultrasonic; ≥89.4 mg/mL in H2O with ultrasonic
Chemical Name4-amino-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2-one
SDFDownload SDF
Canonical SMILESC1C(OC(S1)CO)N2C=CC(=NC2=O)N
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Protocol

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.

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