Home DNA Damage/DNA Repair DNA/RNA Synthesis inhibitor Clevudine For research use only.

Clevudine

Synonyms: Levovir,L-FMAU

Clevudine(Levovir,L-FMAU) is an antiviral drug for the treatment of hepatitis B.

Clevudine Chemical Structure

Clevudine Chemical Structure

CAS: 163252-36-6

Purity & Quality Control

Batch: Purity: 99.96%
99.96

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Biological Activity

Description Clevudine(Levovir,L-FMAU) is an antiviral drug for the treatment of hepatitis B.
Targets
RNA polymerase [1] DNA polymerase [1]
In vitro
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. Clevudine is metabolized in cells by the cellular thymidine kinase as well as deoxycytidine kinase to its monophosphate, and subsequently to the di- and triphosphate. Clevudine 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] Clevudine results in increase of the amounts of the diphosphate and triphosphate metabolites of these analogs. Clevudine monophosphate (L-FMAUMP) is a poorer substrate than its D-configuration anomer. [2] Clevudine is readily phosphorylated to the corresponding 5'-triphosphate form of the compound in cell culture, which involves the mechanism of action of Clevudine. [3]
In Vivo
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. Clevudine is metabolized in cells by the cellular thymidine kinase as well as deoxycytidine kinase to its monophosphate, and subsequently to the di- and triphosphate. Clevudine 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] Clevudine results in increase of the amounts of the diphosphate and triphosphate metabolites of these analogs. Clevudine monophosphate (L-FMAUMP) is a poorer substrate than its D-configuration anomer. [2] Clevudine is readily phosphorylated to the corresponding 5'-triphosphate form of the compound in cell culture, which involves the mechanism of action of Clevudine. [3]
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

Chemical lnformation & Solubility

Molecular Weight 260.22 Formula

C10H13FN2O5
CAS No. 163252-36-6 SDF Download Clevudine SDF
Smiles CC1=CN(C(=O)NC1=O)C2C(C(C(O2)CO)O)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 52 mg/mL ( (199.83 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 52 mg/mL

Ethanol : 4 mg/mL


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In vivo
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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

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