Telbivudine
For research use only.
Catalog No.S1651
2 publications
CAS No. 3424-98-4
Telbivudine is a potent, and selective HBV reverse transcriptase inhibitor, used to treat HBV infection.
Selleck's Telbivudine has been cited by 2 publications
Purity & Quality Control
Choose Selective Reverse Transcriptase Inhibitors
Biological Activity
| Description | Telbivudine is a potent, and selective HBV reverse transcriptase inhibitor, used to treat HBV infection. | |
|---|---|---|
| Targets |
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| 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 |
| Smiles | CC1=CN(C(=O)NC1=O)C2CC(C(O2)CO)O |
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 | ul | |
Number of animals | |
| Step 2: Enter the in vivo formulation () | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
| CalculateReset | ||||||||||
Calculation results:
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
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.
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.
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity 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 |
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.
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