1. Anti-infection
  2. HIV Reverse Transcriptase HBV
  3. Lamivudine

Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS.

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Lamivudine Chemical Structure

Lamivudine Chemical Structure

CAS No. : 134678-17-4

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10 mM * 1 mL in DMSO
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500 mg USD 262 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Lamivudine:

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Description

Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS[1][2].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

229.26

Formula

C8H11N3O3S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC[C@H]1SC[C@@H](N2C(N=C(N)C=C2)=O)O1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (218.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 50 mg/mL (218.09 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.3619 mL 21.8093 mL 43.6186 mL
5 mM 0.8724 mL 4.3619 mL 8.7237 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (10.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (10.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (436.19 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 4.3619 mL 21.8093 mL 43.6186 mL 109.0465 mL
5 mM 0.8724 mL 4.3619 mL 8.7237 mL 21.8093 mL
10 mM 0.4362 mL 2.1809 mL 4.3619 mL 10.9047 mL
15 mM 0.2908 mL 1.4540 mL 2.9079 mL 7.2698 mL
20 mM 0.2181 mL 1.0905 mL 2.1809 mL 5.4523 mL
25 mM 0.1745 mL 0.8724 mL 1.7447 mL 4.3619 mL
30 mM 0.1454 mL 0.7270 mL 1.4540 mL 3.6349 mL
40 mM 0.1090 mL 0.5452 mL 1.0905 mL 2.7262 mL
50 mM 0.0872 mL 0.4362 mL 0.8724 mL 2.1809 mL
60 mM 0.0727 mL 0.3635 mL 0.7270 mL 1.8174 mL
80 mM 0.0545 mL 0.2726 mL 0.5452 mL 1.3631 mL
100 mM 0.0436 mL 0.2181 mL 0.4362 mL 1.0905 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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