GLPBio

Lamivudine

Catalog No.: GC10317Purity:>98.00%Synonyms: (-)-BCH 189, 3TC, 2’,3’-dideoxy-3’-Thiacytidine
COASDSData Sheet
Lamivudin (BCH-189) ist ein oral aktiver nukleosidischer Reverse-Transkriptase-Hemmer (NRTI).

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Lamivudine
Cas No.: 134678-17-4
10mM (in 1mL DMSO)In Stock
$31.00
1
25mgIn Stock
$28.00
1
50mgIn Stock
$40.00
1
100mgIn Stock
$55.00
1
500mgIn Stock
$139.00
1
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Beschreibung (Description)

Lamivudine is an oral nucleoside analogue, which acts as the nucleoside reverse transcriptase inhibitor, with an EC50 of 0.07±0.02μg/ml for anti-hepatitis B virus (HBV) activity[1]. Lamivudine undergoes anabolic phosphorylation by intracellular kinases to form Lamivudine 5′-triphosphate, the active anabolite which prevents HIV-1 and HBV replication by competitively inhibiting viral reverse transcriptase and terminating proviral DNA chain extension [2]. Lamivudine has been used in viral and antitumor studies in various cell and animal models[3].

In vitro, Lamivudine treatment at 300μM in HepG2.2.15 cells for 72 hours significantly reduced the expression of MMP-9, HBsAg, HBeAg, and inhibited the replication of HBV[4]. Treatment of 4μg/ml Lamivudine for 6 days significantly inhibted SDAU1005 virus replication in chick embryo fibroblasts (CEFs) without affecting cell viability[5]. Lamivudine treatment with 500μM for 8 days can stimulate the proliferation of dendritic cells (DC) derived from patients with chronic hepatitis B (CHB), promote the secretion of IL-12 and IL-6, and restore cellular immune function[6].

In vivo, Lamivudine treatment via daily gastric infusion (100mg/kg) in senescence-accelerated mouse prone 8 (SAMP8) mice for 4 weeks significantly improved the ageing status of the mice and alleviated the decline in cognitive ability[7]. Oral administration of 2mg/kg Lamivudine daily for one week reduced the severity of gastric ulcers in a mouse model of ethanol-induced gastric ulcers, and improved the histological features of the gastric mucosa and maintained the integrity of the gastric mucosal barrier[8].

References:
[1] Ying, Clercq D, Neyts. Lamivudine, adefovir and tenofovir exhibit long‐lasting anti‐hepatitis B virus activity in cell culture[J]. Journal of viral hepatitis, 2000, 7(1): 79-83.
[2] Perry C M, Faulds D. Lamivudine: a review of its antiviral activity, pharmacokinetic properties and therapeutic efficacy in the management of HIV infection[J]. Drugs, 1997, 53(4): 657-680.
[3] Johnson M A, Moore K H P, Yuen G J, et al. Clinical pharmacokinetics of lamivudine[J]. Clinical pharmacokinetics, 1999, 36(1): 41-66.
[4] Zhang J, Yu H, Sun F Y, et al. Effects of lamivudine on cell proliferation of liver cancer and expressions of HBsAg, HBeAg, and MMP-9 in patients[J]. Eur. Rev. Med. Pharmacol. Sci, 2019, 23: 9093-9098.
[5] Wang Y, Xu S, Li S, et al. Lamivudine inhibits the replication of ALV-J associated acutely transforming virus and its helper virus and tumor growth in vitro and in vivo[J]. Frontiers in Microbiology, 2015, 6: 1306.
[6] Zheng P Y, Zhang D Y, Lu G F, et al. Effects of lamivudine on the function of dendritic cells derived from patients with chronic hepatitis B virus infection[J]. World Journal of Gastroenterology: WJG, 2007, 13(34): 4641.
[7] Li M, Zhao J, Tang Q, et al. Lamivudine improves cognitive decline in SAMP8 mice: Integrating in vivo pharmacological evaluation and network pharmacology[J]. Journal of Cellular and Molecular Medicine, 2021, 25(17): 8490-8503.
[8] Meng X, Liu J, Kang J, et al. Lamivudine protects mice from gastric ulcer by activating PGK1 to suppress ferroptosis[J]. Biochemical Pharmacology, 2024, 227: 116440.

Protokoll (Protocol)

Cell experiment [1]:

Cell lines

HepG2.2.15 cells

Preparation Method

The HepG2.2.15 cells were cultured with a culture solution of 10% fetal bovine serum in a 37°C incubator with 5% CO2 concentration. They were washed with PBS after 85% of the cells were attached. Then the cells were digested with 1ml of 25% trypsin, and cultured with a concentration of 10% in a culture solution for 48h at 37°C with 5% CO2 concentration for subculture. The cells and supernatants were collected after 72h of Lamivudine intervention (100, 200, and 300μM). The cells were digested with trypsin and centrifuged at 8000r/min for 3min. The supernatant was then discarded, and the cells were collected and resuspended with 200μL of PBS before the detection. The MMP-9, HBsAg, and HBeAg levels were detected using ELISA method.

Reaction Conditions

100, 200, and 300μM; 72h

Applications

Lamivudine treatment significantly inhibited the MMP-9, HBsAg, and HBeAg levels in dose-dependent manner within HepG2.2.15 cells.
Animal experiment [2]:

Animal models

Kunming mice

Preparation Method

Healthy male Kunming mice, 4 weeks old (20±2g), were housed in appropriate cages and allowed to adapt to the laboratory environment for one week. The environmental temperature was maintained at 25°C, and the daily light-dark cycle was 12 hours. The animals had free access to water and standard feed pellets. The mice were randomly divided into 4 groups (n = 8). The control group (Control) and the ethanol group (Ethanol) were given 0.9% physiological saline (1mL/100g/day); the positive drug group (CIM) was orally administered cimetidine (80mg/kg/day); the Lamivudine group was orally administered 2mg/kg/day of Lamivudine. The mice were treated continuously for 1 week. Approximately 2 hours after the last administration, the mice were fasted for 24 hours without restricting water intake. The mice in the ethanol group, the ethanol + CIM group, and the ethanol + Lamivudine (2mg/kg) group (1mL/100g body weight) were intragastrically administered anhydrous ethanol. Meanwhile, the remaining mice were intragastrically administered the same volume of physiological saline. 2 hours later, the mice were dislocated at the cervical vertebra and sacrificed, and the gastric tissues were collected for further biochemical and histopathological examinations.

Dosage form

2mg/kg/day for 7 days; p.o.

Applications

Lamivudine treatment improved histopathological features of gastric mucosa in mice under ethanol stress.

References:
[1] Zhang J, Yu H, Sun F Y, et al. Effects of lamivudine on cell proliferation of liver cancer and expressions of HBsAg, HBeAg, and MMP-9 in patients[J]. Eur. Rev. Med. Pharmacol. Sci, 2019, 23: 9093-9098.
[2] Meng X, Liu J, Kang J, et al. Lamivudine protects mice from gastric ulcer by activating PGK1 to suppress ferroptosis[J]. Biochemical Pharmacology, 2024, 227: 116440.

Produktdokumente (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemische Eigenschaften (Chemical Properties)

CAS-Nr.
134678-17-4
Synonyme
(-)-BCH 189, 3TC, 2’,3’-dideoxy-3’-Thiacytidine
Chemischer Name
4-amino-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2-one
SMILES
C1C(OC(S1)CO)N2C=CC(=NC2=O)N
Summenformel
C8H11N3O3S
Molekulargewicht
229.26
Löslichkeit
≥ 10.5mg/mL in DMSO
Lagerung
Store at -20°C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.

Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit

g/mol

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