1. Anti-infection Metabolic Enzyme/Protease
  2. HCV Protease
  3. Voxilaprevir

Voxilaprevir  (Synonyms: GS-9857)

製品番号: HY-19840 純度: 99.92%
COA 取扱説明書 Technical Support

Voxilaprevir (GS-9857) is a noncovalent, reversible inhibitor of HCV NS3/4A protease inhibitor (PI) with pangenotypic antiviral activity. Voxilaprevir inhibits genotype 1b and 3a wild-type NS3 proteases with Ki values of 0.038 nM and 0.066 nM, respectively. Voxilaprevir is an orally active direct-acting antiviral agent (DAA) and can be used for HCV infection research.

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Voxilaprevir

Voxilaprevir 構造式

CAS 番号 : 1535212-07-7

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 765 在庫あり
Solution
10 mM * 1 mL in DMSO USD 765 在庫あり
Solid
1 mg $90 在庫あり
5 mg $400 在庫あり
10 mg $570 在庫あり
25 mg $950 在庫あり
50 mg $1285 在庫あり
100 mg $1740 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

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製品説明

Voxilaprevir (GS-9857) is a noncovalent, reversible inhibitor of HCV NS3/4A protease inhibitor (PI) with pangenotypic antiviral activity[1]. Voxilaprevir inhibits genotype 1b and 3a wild-type NS3 proteases with Ki values of 0.038 nM and 0.066 nM, respectively[1]. Voxilaprevir is an orally active direct-acting antiviral agent (DAA) and can be used for HCV infection research[2].

IC50 & Target

Hepatitis C virus (HCV) nonstructural protein (NS) 3/4A protease[1]

体外実験

NS3/4A protease is essential for proteolytic cleavage of the HCV encoded polyprotein (intomature forms of NS3, NS4A, NS4B, NS5A and NS5B proteins) and hence for viral replication[1].
In enzymatic assays using recombinant NS3 protease domains and isogenic NS4A peptide cofactors provided in trans. Voxilaprevir is against HCV genotype 1b and 3a NS3 proteases with Ki values of 0.038 nM and 0.066 nM, respectively[1].
In stable cell lines (Huh-7-Lunet or Huh7-1C cells) expressing renilla luciferase-encoding HCV replicons. Voxilaprevir exhibits potent pangenotypic antiviral activity with EC50 ranging from 0.33 to 6.6 nM across genotypes 1 to 6. Voxilaprevir is against HCV replicon strain DQ314805, H77, Con1, JFH-1, J6,J8 (full length) and HM568433, SA13 (NS3 Chimera) with IC50 values of 0.33 nM, 3.9 nM, 3.3 nM, 3.7 nM, 4.5 nM, 1.8 nM, and 6.6 nM, 1.9 nM, respectively[1].

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

臨床実験
分子量

868.93

分子式

C40H52F4N6O9S

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@H]1N(C([C@@H](NC(O[C@H]2[C@H]3C2)=O)C(C)(C)C)=O)C[C@@](OC4=NC5=CC(OC)=CC=C5N=C4C(F)(CCCC3)F)([H])[C@H]1CC)N[C@]6([C@H](C(F)F)C6)C(NS(=O)(C7(CC7)C)=O)=O

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 : ≥ 100 mg/mL (115.08 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 1.1508 mL 5.7542 mL 11.5084 mL
5 mM 0.2302 mL 1.1508 mL 2.3017 mL
10 mM 0.1151 mL 0.5754 mL 1.1508 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.88 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 99.92%

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1508 mL 5.7542 mL 11.5084 mL 28.7710 mL
5 mM 0.2302 mL 1.1508 mL 2.3017 mL 5.7542 mL
10 mM 0.1151 mL 0.5754 mL 1.1508 mL 2.8771 mL
15 mM 0.0767 mL 0.3836 mL 0.7672 mL 1.9181 mL
20 mM 0.0575 mL 0.2877 mL 0.5754 mL 1.4386 mL
25 mM 0.0460 mL 0.2302 mL 0.4603 mL 1.1508 mL
30 mM 0.0384 mL 0.1918 mL 0.3836 mL 0.9590 mL
40 mM 0.0288 mL 0.1439 mL 0.2877 mL 0.7193 mL
50 mM 0.0230 mL 0.1151 mL 0.2302 mL 0.5754 mL
60 mM 0.0192 mL 0.0959 mL 0.1918 mL 0.4795 mL
80 mM 0.0144 mL 0.0719 mL 0.1439 mL 0.3596 mL
100 mM 0.0115 mL 0.0575 mL 0.1151 mL 0.2877 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:
Voxilaprevir
製品番号:
HY-19840
数量:
MCE 日本正規代理店: