Telbivudine

Synonyms: NV 02B

Telbivudine(NV 02B) is a potent, and selective HBV reverse transcriptase inhibitor, used to treat HBV infection.

Telbivudine  Chemical Structure

Telbivudine Chemical Structure

CAS: 3424-98-4

Selleck's Telbivudine has been cited by 3 publications

Purity & Quality Control

Batch: Purity: 99.95%
99.95

Choose Selective Reverse Transcriptase Inhibitors

Biological Activity

Description Telbivudine(NV 02B) is a potent, and selective HBV reverse transcriptase inhibitor, used to treat HBV infection.
Targets
HBV RT [1]
In vitro
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]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02894554 Terminated HBsAg-positive Renal Allograft Recipients National Taiwan University Hospital July 2014 Phase 4
NCT01379508 Completed 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 Compensated Chronic Hepatitis B Novartis Pharmaceuticals|Novartis March 2009 Phase 4
NCT01743079 Completed Chronic Hepatitis B|Late Pregnancy|Transmission|Complication Beijing YouAn Hospital|New Discovery LLC January 2009 Phase 4

Chemical lnformation & Solubility

Molecular Weight 242.23 Formula

C10H14N2O5

CAS No. 3424-98-4 SDF Download Telbivudine SDF
Smiles CC1=CN(C(=O)NC1=O)C2CC(C(O2)CO)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 48 mg/mL ( (198.15 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 48 mg/mL

Ethanol : 2 mg/mL


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

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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