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

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 화학구조

CAS No. : 1535212-07-7

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
1 mg 해외재고보유
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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고객리뷰

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  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

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]

In Vitro

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.

Clinical Trial
분자량

868.93

화학식

C40H52F4N6O9S

CAS No.
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

선적

Room temperature in continental US; may vary elsewhere.

보관
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
용액&용해도
In Vitro: 

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
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.

  • 몰농도 계산기

  • 농도 희석 계산기

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.
순도&문서

Purity: 99.92%

References

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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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

상품명:
Voxilaprevir
Cat. No.:
HY-19840
수량:
MCE Japan Authorized Agent: