Telbivudine

Catalog No.S1651

Telbivudine  Chemical Structure

Molecular Weight(MW): 242.23

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

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Biological Activity

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

Solubility (25°C)

In vitro DMSO 48 mg/mL warmed (198.15 mM)
Water 48 mg/mL warmed (198.15 mM)
Ethanol 2 mg/mL warmed (8.25 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 242.23
Formula

C10H14N2O5

CAS No. 3424-98-4
Storage powder
in solvent
Synonyms N/A

Bio Calculators

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

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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

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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Reverse Transcriptase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID