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Telbivudine Reverse Transcriptase inhibitor

Name: Telbivudine
SKU: S1651
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S1651

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

Chemical Structure

Molecular Weight: 242.23

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.95%

99.95

Related Targets	Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite HIV HCV Protease SARS-CoV HIV Protease Influenza Virus β-lactamase Integrase HBV CMV Neuraminidase HCV Thioredoxin Reductase HSV RSV Enterovirus 3C-Like Protease Ribosomal Peptidyl Transferase HPV
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Chemical Information, Storage & Stability

Molecular Weight	242.23	Formula	C₁₀H₁₄N₂O₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	3424-98-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NV 02B			Smiles	CC1=CN(C(=O)NC1=O)C2CC(C(O2)CO)O

Solubility

In vitro
Batch:

DMSO : 48 mg/mL (198.15 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 48 mg/mL

Ethanol : 2 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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.

Mechanism of Action

Targets/IC₅₀/Ki	HBV RT ^[1]
In vitro	Telbivudine shows potent, selective, and specific antiviral activity against HBV and other hepadna viruses. This compound is phosphorylated by intracellular thymidine kinases to the active triphosphate form, which has an intracellular half-life of 14 hours. Its 5′-triphosphate inhibits HBV DNA polymerase (reverse transcriptase) by competing with the natural substrate, dTTP. ^[1] This chemical significantly increases the production of tumour necrosis factor-alpha and interleukin-12 in MHV-3-induced macrophages. It significantly elevates serum levels of interferon-gamma. This treatment enhances the ability of T cells to undergo proliferation and secrete cytokines but does not affect cytotoxicity of infected hepatocytes. It suppresses programmed death ligand 1 expression on T cells. ^[2] The compound remains active as shown by respective fold-changes of 0.5 (N236T) and 1.0 (A181V and A194T). It 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]
References	[1] https://pubmed.ncbi.nlm.nih.gov/18474576/ [2] https://pubmed.ncbi.nlm.nih.gov/20586931/ [3] https://pubmed.ncbi.nlm.nih.gov/19028525/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
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

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