Art. -Nr.: HY-19447

Besifovir

(Synonyms: LB80331)

1 Cited Publications

Kundenbewertung

Based on 1 publication(s) in Google Scholar

Besifovir (LB80331), a parent agent converted by LB80380 (HY-19447A), further metabolizes to its active form, LB80317 (HY-106235). Besifovir is an orally active, novel antiviral agent against hepatitis B virus (HBV).

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Reinheit: 98.0%
CAS. Nr.: 441785-25-7
Formel: C₁₀H₁₄N₅O₄P
Molecular Weight:299.22

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Besifovir Chemical Structure

CAS. Nr.: 441785-25-7

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	EC₅₀	4 μM Compound: 8	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: 8	Cytotoxic activity in HepG2 2.2.15 cell line Cytotoxic activity in HepG2 2.2.15 cell line	[PMID: 15139764]

In Vivo

The prodrug, LB80380, is rapidly absorbed after oral administration (30, 60, 120, 240 mg) and is converted to its parent drug, Besifovir (LB80331) (LB80380 was not detected in plasma). The median T_maxs of LB80331 ranged from 1.0 to 2.0 h postdosing. Thereafter, the plasma LB80331 concentration declined in a monoexponential manner, and the mean values of t_1/2 ranged from 2.5 to 3.3 h^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 441785-25-7
Appearance Solid
Molecular Weight 299.22
Formel C₁₀H₁₄N₅O₄P
Color Light yellow to yellow
SMILES

NC1=NC=C2N=CN(CC3(OCP(O)(O)=O)CC3)C2=N1
Synonyms

LB80331
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Journal Impact Factor

J Med Virol

Monkeypox Virus Is Inhibited by Nucleoside Analogues Including the Acyclic Phosphonates Adefovir and Tenofovir In Vitro. [Abstract]

2025 Nov;97(11):e70669. PMID: 41137742

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 250 mg/mL (835.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 100 mg/mL (334.20 mM)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.3420 mL

16.7101 mL

33.4202 mL

5 mM

0.6684 mL

3.3420 mL

6.6840 mL

10 mM

0.3342 mL

1.6710 mL

3.3420 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (6.95 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (6.95 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (6.95 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Jung JA, et al. Pharmacokinetic comparison of the maleate and free base formulations of LB80380, a novel nucleotide analog, in healthy male volunteers. Int J Clin Pharmacol Ther. 2012 Sep;50(9):657-64. [Content Brief]

[2]. Yuen MF, et al. A randomized placebo-controlled, dose-finding study of oral LB80380 in HBeAg-positive patients with chronic hepatitis B. Antivir Ther. 2006;11(8):977-83. [Content Brief]

[3]. 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	3.3420 mL	16.7101 mL	33.4202 mL	83.5506 mL
	5 mM	0.6684 mL	3.3420 mL	6.6840 mL	16.7101 mL
	10 mM	0.3342 mL	1.6710 mL	3.3420 mL	8.3551 mL
	15 mM	0.2228 mL	1.1140 mL	2.2280 mL	5.5700 mL
	20 mM	0.1671 mL	0.8355 mL	1.6710 mL	4.1775 mL
	25 mM	0.1337 mL	0.6684 mL	1.3368 mL	3.3420 mL
	30 mM	0.1114 mL	0.5570 mL	1.1140 mL	2.7850 mL
	40 mM	0.0836 mL	0.4178 mL	0.8355 mL	2.0888 mL
	50 mM	0.0668 mL	0.3342 mL	0.6684 mL	1.6710 mL
	60 mM	0.0557 mL	0.2785 mL	0.5570 mL	1.3925 mL
	80 mM	0.0418 mL	0.2089 mL	0.4178 mL	1.0444 mL
	100 mM	0.0334 mL	0.1671 mL	0.3342 mL	0.8355 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Besifovir

1 Cited Publications

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Besifovir

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Publications Citing Use of MedChemExpress (MCE) Besifovir

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Besifovir

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Human Metabolite Library

Off-patent Drug Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Infection Compound Library

FDA-Approved Drug Library

Antiviral Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) Besifovir

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Besifovir Related Classifications

HY-19447 Related Classifications