LB80317
LB80317 is an active metabolite of LB80380 and suppresses the DNA synthesis of HBV with an EC50 of 0.5 μM. LB80317 has antiviral effect and has the potential for chronic hepatitis B treatment.
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- CAS No.: 441785-24-6
- 화학식: C10H14N5O5P
- 분자량:315.22
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All DNA/RNA Synthesis Isoforms
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Biological Activity
제품 설명
IC50 & Target
EC50: 0.5 μM (DNA synthesis of HBV)[2]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | EC50 |
0.5 μM
Compound: 1
|
Compound tested for anti-HBV (hepatitis B virus) activity in HepG2 2.2.15 cell line
Compound tested for anti-HBV (hepatitis B virus) activity in HepG2 2.2.15 cell line
|
[PMID: 15139764] |
| HepG2 | CC50 |
>1000 μM
Compound: 1
|
Cytotoxic activity in HepG2 2.2.15 cell line
Cytotoxic activity in HepG2 2.2.15 cell line
|
[PMID: 15139764] |
In Vitro
After phosphorylation to di- and triphosphate forms, LB80317 is incorporated into the viral DNA inside the nucleocapsid, which inhibits further DNA synthesis. In in vitro studies using cell line models, the drug concentrations causing 50% reduction in HBV DNA produced (EC50) is 0.5 μM for LB80317[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 441785-24-6
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분자량 315.22
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화학식 C10H14N5O5P
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SMILES
OP(O)(COC1(CN2C=NC3=C2N=C(N)NC3=O)CC1)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
The EdU incorporation assay measures DNA synthesis by adding the thymidine analog 5-ethynyl-2′-deoxyuridine to cells or tissues, where it is incorporated into newly synthesized DNA during S phase. Incorporated EdU is detected by copper-catalyzed azide-alkyne cycloaddition, in which a fluorescent azide covalently reacts with the ethynyl group on EdU, allowing S-phase cells to be detected by fluorescence microscopy, flow cytometry, or high-content imaging. EdU detection does not require DNA denaturation or anti-BrdU antibody access, which preserves sample structure and improves compatibility with immunostaining and multiparameter cytometry compared with BrdU-based detection. EdU can be cytotoxic in a cell-type- and exposure-dependent manner, so pulse duration, concentration, and continuous-labeling designs should be validated for each cell type.
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
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BrdU Incorporation Assay
Bromodeoxyuridine (BrdU) incorporation assay is based on the principle that BrdU, a thymidine analog, is incorporated into newly synthesized DNA during the S phase of the cell cycle, thereby serving as a marker of DNA replication and cellular proliferation. Incorporated BrdU can be detected using anti-BrdU antibodies following DNA denaturation, enabling visualization or quantification of proliferating cells through immunochemical detection methods such as immunofluorescence or immunohistochemistry.
순도&문서
References
[1]. Man-Fung Yuen, et al. Pharmacokinetics of LB80331 and LB80317 Following Oral Administration of LB80380, a New Antiviral Agent for Chronic Hepatitis B (CHB), in Healthy Adult Subjects, CHB Patients, and Mice. Antimicrob Agents Chemother. 2009 May;53(5):177 [Content Brief]
[2]. Lung-Yi Mak, et al. Pharmacokinetic Evaluation of Besifovir for the Treatment of HBV Infection. Expert Opin Drug Metab Toxicol. 2018 Jan;14(1):101-106. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)