Besifovir
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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.0%
- CAS 番号: 441785-25-7
- 分子式: C10H14N5O4P
- 分子量:299.22
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 Besifovir
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | EC50 |
4 μM
Compound: 8
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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
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[PMID: 15139764] |
| HepG2 | CC50 |
>1000 μM
Compound: 8
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Cytotoxic activity in HepG2 2.2.15 cell line
Cytotoxic activity in HepG2 2.2.15 cell line
|
[PMID: 15139764] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 441785-25-7
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性状 Solid
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分子量 299.22
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分子式 C10H14N5O4P
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Color Light yellow to yellow
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SMILES
NC1=NC=C2N=CN(CC3(OCP(O)(O)=O)CC3)C2=N1
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別名
LB80331
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
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Most Recent
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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
溶剤 & 溶解度
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.
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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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.
純度とドキュメンテーション
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データシート (277 KB)
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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)
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取扱説明書 (2659 KB)
参考文献
[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]
Complete Stock Solution Preparation Table
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.
| 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.