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Telbivudine

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

Synonyms: NV 02B

Catalog No.S1651 Purity:99.95%

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

Telbivudine Chemical Structure

CAS No. 3424-98-4

Purity & Quality Control

Batch: Purity: 99.95%

99.95

Telbivudine Related Products

Related Targets	HBV RT HIV RT RT	Click to Expand
Related Products	Dapivirine (TMC120) Salicylanilide Fangchinoline	Click to Expand
Related Compound Libraries	Anti-infection Compound Library Antibiotics compound Library Antiviral Compound Library Anti-parasitic Compound Library Gut Microbial Metabolite Library	Click to Expand

Signaling Pathway

Reverse Transcriptase Signaling Pathway

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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT02956850	Completed	Hepatitis B Chronic	Hoffmann-La Roche	December 12 2016	Phase 1
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

References

Chemical Information & 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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

%DMSO+ %

Calculation results:

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

Tel: +1-832-582-8158 Ext:3
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