1. Cell Cycle/DNA Damage Anti-infection
  2. DNA/RNA Synthesis HCV
  3. Beclabuvir

Beclabuvir  (Synonyms: BMS-791325)

製品番号: HY-12429 純度: 99.94%
COA 取扱説明書 Technical Support

Beclabuvir is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, and inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 with IC50 of < 28 nM.

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Beclabuvir

Beclabuvir 構造式

CAS 番号 : 958002-33-0

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 610 在庫あり
Solution
10 mM * 1 mL in DMSO USD 610 在庫あり
Solid
1 mg $168 在庫あり
5 mg $420 在庫あり
10 mg $660 在庫あり
25 mg $1320 在庫あり
50 mg $1920 在庫あり
100 mg $2880 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 5 publication(s) in Google Scholar

Other Forms of Beclabuvir:

Top Publications Citing Use of Products

DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示:

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

Beclabuvir is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, and inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 with IC50 of < 28 nM[1][2].

IC50 & Target

RNA Polymerase

 

Cellular Effect
Cell Line Type Value Description References
HepG2 EC50
>50 μM
Compound: 2, BMS-791325
Transactivation of human PXR expressed in human HepG2 cells by luciferase reporter gene assay
Transactivation of human PXR expressed in human HepG2 cells by luciferase reporter gene assay
[PMID: 24397558]
Huh-7 CC50
>10 μM
Compound: 2, BMS-791325
Cytotoxicity against human HuH7 cells by Alamar blue assay
Cytotoxicity against human HuH7 cells by Alamar blue assay
[PMID: 24397558]
Huh-7 CC50
16 μM
Compound: 1
Cytotoxicity against human HuH7 cells after 4 hrs by CellTitre-Blue assay
Cytotoxicity against human HuH7 cells after 4 hrs by CellTitre-Blue assay
[PMID: 24656612]
Huh-7 EC50
0.003 μM
Compound: 2, BMS-791325
Antiviral activity against Hepatitis C virus H77c genotype 1a infected in human HuH7 cells after 3 days by FRET assay
Antiviral activity against Hepatitis C virus H77c genotype 1a infected in human HuH7 cells after 3 days by FRET assay
[PMID: 24397558]
Huh-7 EC50
0.006 μM
Compound: 2, BMS-791325
Antiviral activity against Hepatitis C virus Con1 genotype 1b infected in human HuH7 cells after 3 days by FRET assay
Antiviral activity against Hepatitis C virus Con1 genotype 1b infected in human HuH7 cells after 3 days by FRET assay
[PMID: 24397558]
Huh-7 EC50
0.028 μM
Compound: 2, BMS-791325
Antiviral activity against Hepatitis C virus Con1 genotype 1b infected in human HuH7 cells after 3 days by FRET assay in presence of 40% human serum
Antiviral activity against Hepatitis C virus Con1 genotype 1b infected in human HuH7 cells after 3 days by FRET assay in presence of 40% human serum
[PMID: 24397558]
Huh-7 EC50
2 nM
Compound: 1
Antiviral activity against HCV genotype 1a H77c infected in human HuH7 cells after 3 days by luciferase reporter gene assay
Antiviral activity against HCV genotype 1a H77c infected in human HuH7 cells after 3 days by luciferase reporter gene assay
[PMID: 24656612]
体外実験

Beclabuvir demonstrates additive or synergistic antiviral activity with pegIFN/RBV and in 2- or 3-drug combinations with a range of DAAs, such as HCV NS3 protease inhibitors, NS5A inhibitors' and/or nucleoside NS5B inhibitors[2].

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

体内実験

The combination of beclabuvir with asunaprevir and daclatasvir achieves very high rates of viral eradication (about 90%) in patients infected with HCV genotype 1, which is the most common genotype worldwide[1].

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

分子量

659.84

分子式

C36H45N5O5S

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1C2CCC1CN(C)C2)[C@@]3(CN4C5=C(C6CCCCC6)C7=CC=C(C(NS(=O)(N(C)C)=O)=O)C=C47)[C@H](C8=CC(OC)=CC=C85)C3

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 30 mg/mL (45.47 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5155 mL 7.5776 mL 15.1552 mL
5 mM 0.3031 mL 1.5155 mL 3.0310 mL
10 mM 0.1516 mL 0.7578 mL 1.5155 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

C1

×
体積 (開始)

V1

=
濃度 (終了)

C2

×
体積 (終了)

V2

体内:

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.

  • Protocol 1

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

    Solubility: ≥ 2.5 mg/mL (3.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (3.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.94%

参考文献

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
DMSO 1 mM 1.5155 mL 7.5776 mL 15.1552 mL 37.8880 mL
5 mM 0.3031 mL 1.5155 mL 3.0310 mL 7.5776 mL
10 mM 0.1516 mL 0.7578 mL 1.5155 mL 3.7888 mL
15 mM 0.1010 mL 0.5052 mL 1.0103 mL 2.5259 mL
20 mM 0.0758 mL 0.3789 mL 0.7578 mL 1.8944 mL
25 mM 0.0606 mL 0.3031 mL 0.6062 mL 1.5155 mL
30 mM 0.0505 mL 0.2526 mL 0.5052 mL 1.2629 mL
40 mM 0.0379 mL 0.1894 mL 0.3789 mL 0.9472 mL
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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

製品名:
Beclabuvir
製品番号:
HY-12429
数量:
MCE 日本正規代理店: