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Telbivudine

Name: Telbivudine
Brand: Selleck Chemicals
SKU: S1651
Rating: 5 (3 reviews)

Catalog No.S1651

For research use only.

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

CAS No. 3424-98-4

Selleck's Telbivudine has been cited by 3 Publications

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Reverse Transcriptase Signaling Pathways

Reverse Transcriptase Signaling Pathway Map

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)

References

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight	242.23
Formula	C₁₀H₁₄N₂O₅
CAS No.	3424-98-4
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CC1=CN(C(=O)NC1=O)C2CC(C(O2)CO)O

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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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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.

Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

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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