Telbivudine

Catalog No.S1651

For research use only.

Telbivudine is a potent, and selective HBV reverse transcriptase inhibitor, used to treat HBV infection.

Telbivudine  Chemical Structure

CAS No. 3424-98-4

Selleck's Telbivudine has been cited by 3 Publications

Purity & Quality Control

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Biological Activity

Description Telbivudine is a potent, and selective HBV reverse transcriptase inhibitor, used to treat HBV infection.
Targets
HBV RT [1]
In vitro

Telbivudine shows potent, selective, and specific antiviral activity against HBV and other hepadna viruses. Telbivudine is phosphorylated by intracellular thymidine kinases to the active triphosphate form, which has an intracellular half-life of 14 hours. Telbivudine 5′-triphosphate inhibits HBV DNA polymerase (reverse transcriptase) by competing with the natural substrate, dTTP. [1] Telbivudine significantly increases the production of tumour necrosis factor-alpha and interleukin-12 in MHV-3-induced macrophages. Telbivudine significantly elevates serum levels of interferon-gamma. Telbivudine treatment enhances the ability of T cells to undergo proliferation and secrete cytokines but does not affect cytotoxicity of infected hepatocytes. Telbivudine treatment suppresses programmed death ligand 1 expression on T cells. [2] Telbivudine remains active as shown by respective fold-changes of 0.5 (N236T) and 1.0 (A181V and A194T). Telbivudine is not active against HBV strains bearing lamivudine mutations L180M/M204V/I but remains active against the M204V single mutant in vitro, potentially explaining the difference in resistance profiles between telbivudine and lamivudine. [3]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 242.23
Formula

C10H14N2O5

CAS No. 3424-98-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CN(C(=O)NC1=O)C2CC(C(O2)CO)O

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02894554 Terminated Drug: Telbivudine|Drug: Lamivudine HBsAg-positive Renal Allograft Recipients National Taiwan University Hospital July 2014 Phase 4
NCT01379508 Completed Drug: telbivudine|Drug: tenofovir disoproxil fumarate Chronic Hepatitis B Novartis Pharmaceuticals|Novartis March 21 2011 Phase 4
NCT01163240 Completed -- Liver Diseases|Hepatitis Chronic|Hepatitis Viral Human|Hepatitis|Virus Diseases|Digestive System Diseases|Hepatitis B Chronic|Hepatitis B|DNA Virus Infections Novartis Pharmaceuticals|Novartis June 2009 --
NCT00877149 Completed Drug: telbivudine/LDT600 Compensated Chronic Hepatitis B Novartis Pharmaceuticals|Novartis March 2009 Phase 4
NCT01743079 Completed Drug: Telbivudine|Drug: Lamivudine Chronic Hepatitis B|Late Pregnancy|Transmission|Complication Beijing YouAn Hospital|New Discovery LLC January 2009 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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