Art. -Nr.: HY-75800

Lomibuvir

(Synonyms: VX-222)

2 Cited Publications

Kundenbewertung

Based on 2 publication(s) in Google Scholar

Lomibuvir (VX-222), a selective, non-nucleoside polymerase inhibitor, targets thumb pocket 2 of the HCV NS5B polymerase (RdRp) with a K_d of 17 nM. Lomibuvir inhibits the 1b/Con1 HCV subgenomic replicon with an EC₅₀ of 5.2 nM. Lomibuvir preferentially inhibits elongative RNA synthesis rather than de novo-initiated RNA synthesis.

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Reinheit: 99.71%
CAS. Nr.: 1026785-55-6
Formel: C₂₅H₃₅NO₄S
Molecular Weight:445.61

Speicherung:

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

Lomibuvir Chemical Structure

CAS. Nr.: 1026785-55-6

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Huh-7	CC₅₀	>20 μM Compound: 1	Cytotoxicity against human Huh-7 cells transfected with HCV subgenomic replicon for NS5B polymerase assessed as reduction in cell viability Cytotoxicity against human Huh-7 cells transfected with HCV subgenomic replicon for NS5B polymerase assessed as reduction in cell viability	[PMID: 28197321]
Huh-7	CC₅₀	>=20 μM Compound: 3, Lomibuvir	Cytotoxicity against human HuH7 cells after 3 days by Cell Titre Glo assay Cytotoxicity against human HuH7 cells after 3 days by Cell Titre Glo assay	[PMID: 24144213]
Huh-7	EC₅₀	13 nM Compound: 3, Lomibuvir	Antiviral activity against Hepatitis C virus H77 genotype 1a infected in human HuH7 cells assessed as observed antiviral potency after 72 hrs by luciferase reporter gene assay Antiviral activity against Hepatitis C virus H77 genotype 1a infected in human HuH7 cells assessed as observed antiviral potency after 72 hrs by luciferase reporter gene assay	[PMID: 24144213]
Huh-7	EC₅₀	15 nM Compound: lomibuvir	Antiviral activity against Hepatitis C virus genotype 1a infected in human HuH7.5 cells after 3 days by luciferase reporter gene assay Antiviral activity against Hepatitis C virus genotype 1a infected in human HuH7.5 cells after 3 days by luciferase reporter gene assay	[PMID: 23768906]
Huh-7	EC₅₀	2.8 nM Compound: 3, Lomibuvir	Antiviral activity against Hepatitis C virus H77 genotype 1a infected in human HuH7 cells assessed as intrinsic antiviral potency after 72 hrs by luciferase reporter gene assay Antiviral activity against Hepatitis C virus H77 genotype 1a infected in human HuH7 cells assessed as intrinsic antiviral potency after 72 hrs by luciferase reporter gene assay	[PMID: 24144213]
Huh-7	EC₅₀	23 nM Compound: lomibuvir	Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7.5 cells after 3 days by luciferase reporter gene assay Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7.5 cells after 3 days by luciferase reporter gene assay	[PMID: 23768906]
Huh-7	EC₅₀	6 nM Compound: 3, Lomibuvir	Antiviral activity against Hepatitis C virus Con1 genotype 1b infected in human HuH7 cells after 72 hrs by luciferase reporter gene assay Antiviral activity against Hepatitis C virus Con1 genotype 1b infected in human HuH7 cells after 72 hrs by luciferase reporter gene assay	[PMID: 24144213]
MT4	CC₅₀	>20 μM Compound: 3, Lomibuvir	Cytotoxicity against human MT4 cells after 5 days by Cell Titre Glo assay Cytotoxicity against human MT4 cells after 5 days by Cell Titre Glo assay	[PMID: 24144213]

In Vitro

Lomibuvir (VX-222) inhibits WT HCV 1b/Con1 replicon with an EC₅₀ of 5.2 nM. Lomibuvir inhibits M423T, L419M and I482L (mutant replicons) with EC₅₀s of 79.8, 563.1, 45.3 nM, respectively. Lomibuvir reduces de novo initiation slightly but also shows strong inhibition of primer extension. The IC₅₀ of Lomibuvir for primer-extended RNA synthesis is 31 nM^[1].
Lomibuvir is a non-nucleoside, allosteric inhibitor of the hepatitis C virus NS5B polymerase^[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. 1026785-55-6
Appearance Solid
Molecular Weight 445.61
Formel C₂₅H₃₅NO₄S
Color White to off-white
SMILES

O=C(C1=C(N([C@@H]2CC[C@@H](O)CC2)C([C@H]3CC[C@H](C)CC3)=O)C=C(C#CC(C)(C)C)S1)O
Synonyms

VX-222
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 (2)

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Journal Impact Factor

Antiviral Res

Antiviral candidates against the hepatitis E virus (HEV) and their combinations inhibit HEV growth in in vitro. [Abstract]

2019 Oct:170:104570. PMID: 31362004
J Virol Methods

Screening of novel drugs for inhibiting hepatitis E virus replication. [Abstract]

2019 Aug:270:1-11. PMID: 31004661

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (224.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.2441 mL

11.2205 mL

22.4409 mL

5 mM

0.4488 mL

2.2441 mL

4.4882 mL

10 mM

0.2244 mL

1.1220 mL

2.2441 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.

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: 2.5 mg/mL (5.61 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (5.61 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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (5.61 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 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.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 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]. Yi G, Deval J, et al. Biochemical study of the comparative inhibition of hepatitis C virus RNA polymerase by VX-222 and filibuvir. Antimicrob Agents Chemother. 2012;56(2):830-837. [Content Brief]

[2]. Li P, Dorsch W, et al. Discovery of Novel Allosteric HCV NS5B Inhibitors. 2. Lactam-Containing Thiophene Carboxylates. ACS Med Chem Lett. 2017;8(2):251-255. Published 2017 Jan 31. [Content Brief]

[3]. M. Rodriguez-Torres et al. SAFETY AND ANTIVIRAL ACTIVITY OF THE HCV NON-NUCLEOSIDE POLYMERASE INHIBITOR VX-222 IN TREATMENT-NAIVE GENOTYPE 1 HCV-INFECTED PATIENTS Journal of Hepatology Volume 52, Supplement 1 , Page S14, April 2010

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
DMSO	1 mM	2.2441 mL	11.2205 mL	22.4409 mL	56.1023 mL
	5 mM	0.4488 mL	2.2441 mL	4.4882 mL	11.2205 mL
	10 mM	0.2244 mL	1.1220 mL	2.2441 mL	5.6102 mL
	15 mM	0.1496 mL	0.7480 mL	1.4961 mL	3.7402 mL
	20 mM	0.1122 mL	0.5610 mL	1.1220 mL	2.8051 mL
	25 mM	0.0898 mL	0.4488 mL	0.8976 mL	2.2441 mL
	30 mM	0.0748 mL	0.3740 mL	0.7480 mL	1.8701 mL
	40 mM	0.0561 mL	0.2805 mL	0.5610 mL	1.4026 mL
	50 mM	0.0449 mL	0.2244 mL	0.4488 mL	1.1220 mL
	60 mM	0.0374 mL	0.1870 mL	0.3740 mL	0.9350 mL
	80 mM	0.0281 mL	0.1403 mL	0.2805 mL	0.7013 mL
	100 mM	0.0224 mL	0.1122 mL	0.2244 mL	0.5610 mL

Keywords

Lomibuvir

2 Cited Publications

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Lomibuvir

Anti-Hepatitis C Virus Compound Library

Targeted Diversity Library

Human Metabolite Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

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Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Alkyne Compound Library

Anti-Infection Compound Library

Cell Cycle/DNA Damage Compound Library

Clinical Compound Library

Antiviral Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) Lomibuvir

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Lomibuvir

Anti-Hepatitis C Virus Compound Library

Targeted Diversity Library

Human Metabolite Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Alkyne Compound Library

Anti-Infection Compound Library

Cell Cycle/DNA Damage Compound Library

Clinical Compound Library

Antiviral Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) Lomibuvir

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Lomibuvir Related Classifications

HY-75800 Related Classifications