Home DNA Damage/DNA Repair DNA/RNA Synthesis inhibitor Clevudine

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Clevudine DNA/RNA Synthesis inhibitor

Cat.No.S3001

Clevudine(Levovir,L-FMAU) is an antiviral drug for the treatment of hepatitis B.
Clevudine DNA/RNA Synthesis inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 260.22

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Chemical Information, Storage & Stability

Molecular Weight 260.22 Formula

C10H13FN2O5

 Storage (From the date of receipt)
CAS No. 163252-36-6 Download SDF Storage of Stock Solutions

Synonyms Levovir,L-FMAU Smiles CC1=CN(C(=O)NC1=O)C2C(C(C(O2)CO)O)F

Solubility

In vitro
Batch:

DMSO : 52 mg/mL (199.83 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 52 mg/mL

Ethanol : 4 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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.

Mechanism of Action

Targets/IC50/Ki
RNA polymerase [1]
DNA polymerase [1]
In vitro

Clevudine is a potent antiviral agent against HBV (EC50 0.1 μM in HepG2 2.2.15 cells) as well as EBV, which has low cytotoxicities in a variety of cell lines including MT2, CEM, H1 and HepG2 2.2.15 and bone marrow progenitor cells. This compound is metabolized in cells by the cellular thymidine kinase as well as deoxycytidine kinase to its monophosphate, and subsequently to the di- and triphosphate. It is known to act specifically on viral DNA synthesis, and its triphosphate inhibits the HBV DNA synthesis in a dose-dependent manner without being incorporated into the DNA or chain termination. [1] This agent results in increase of the amounts of the diphosphate and triphosphate metabolites of these analogs. Its monophosphate (L-FMAUMP) is a poorer substrate than its D-configuration anomer. [2] It is readily phosphorylated to the corresponding 5'-triphosphate form of the compound in cell culture, which involves the mechanism of action of this chemical. [3]
In vivo

Clevudine is a potent antiviral agent against HBV (EC50 0.1 μM in HepG2 2.2.15 cells) as well as EBV, which has low cytotoxicities in a variety of cell lines including MT2, CEM, H1 and HepG2 2.2.15 and bone marrow progenitor cells. This compound is metabolized in cells by the cellular thymidine kinase as well as deoxycytidine kinase to its monophosphate, and subsequently to the di- and triphosphate. It is known to act specifically on viral DNA synthesis, and its triphosphate inhibits the HBV DNA synthesis in a dose-dependent manner without being incorporated into the DNA or chain termination. [1] This agent results in increase of the amounts of the diphosphate and triphosphate metabolites of these analogs. Its monophosphate (L-FMAUMP) is a poorer substrate than its D-configuration anomer. [2] This chemical is readily phosphorylated to the corresponding 5'-triphosphate form of the compound in cell culture, which involves the mechanism of action of this compound. [3]
References

Clinical Trial Information

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

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05298332 Terminated
Chronic Hepatitis b
Antios Therapeutics Inc
 March 29 2022 Phase 1
NCT05137548 Completed
Drug Interaction
Antios Therapeutics Inc
 October 27 2021 Phase 1
NCT04847440 Terminated
Hepatitis B Chronic|Hepatitis D
Antios Therapeutics Inc
 March 30 2021 Phase 2
NCT04248426 Completed
Hepatitis B Chronic
Antios Therapeutics Inc
 February 5 2020 Phase 1
NCT00558818 Completed
Chronic Hepatitis B
Bukwang Pharmaceutical
 June 2007 Phase 4

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