Velpatasvir
Based on 10 publication(s) in Google Scholar
Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 2.16 μM.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.83%
- CAS No.: 1377049-84-7
- Formule: C49H54N8O8
- Masse moléculaire:883.00
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Anti-Infection Compound Library
HY-L002
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Publications Citing Use of MedChemExpress (MCE) Velpatasvir
More- Signal Transduct Target Ther. 2021 May 29;6(1):212. [Abstract]
- Hepatology. 2019 May;69(5):1861-1872. [Abstract]
- J Gastroenterol. 2019 May;54(5):449-458. [Abstract]
- Pharmaceuticals (Basel). 2022 Feb 18;15(2):242. [Abstract]
- Sci Rep. 2019 Apr 5;9(1):5722. [Abstract]
- Viruses. 2018 Aug 28;10(9). pii: E462. [Abstract]
- Hepatol Res. 2019 Nov;49(11):1275-1285. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2019 Mar 15:1110-1111:15-24. [Abstract]
- PLoS One. 2021 May 20;16(5):e0251934. [Abstract]
- bioRxiv. 2023 Aug 20:2023.08.19.553982. [Abstract]
Activité biologique
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Cell Line
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Type | Value | Description | References |
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| HepG2 | CC50 |
>44400 nM
Compound: 39; VEL, GS-5816
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Cytotoxicity against human HepG2 cells infected with HCV genotype 1a H77 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay
Cytotoxicity against human HepG2 cells infected with HCV genotype 1a H77 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay
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[PMID: 31230974] |
| HepG2 | CC50 |
>44400 nM
Compound: 39; VEL, GS-5816
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Cytotoxicity against human HepG2 cells infected with HCV genotype 1b Con-1 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay
Cytotoxicity against human HepG2 cells infected with HCV genotype 1b Con-1 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay
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[PMID: 31230974] |
| Huh-7 | CC50 |
>44400 nM
Compound: 39; VEL, GS-5816
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Cytotoxicity against human HuH7 cells infected with HCV genotype 1a H77 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay
Cytotoxicity against human HuH7 cells infected with HCV genotype 1a H77 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay
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[PMID: 31230974] |
| Huh-7 | CC50 |
>44400 nM
Compound: 39; VEL, GS-5816
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Cytotoxicity against human HuH7 cells infected with HCV genotype 1b Con-1 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay
Cytotoxicity against human HuH7 cells infected with HCV genotype 1b Con-1 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay
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[PMID: 31230974] |
| MRC5 | CC50 |
>44400 nM
Compound: 39; VEL, GS-5816
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Cytotoxicity against human MRC5 cells infected with HCV genotype 1a H77 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay
Cytotoxicity against human MRC5 cells infected with HCV genotype 1a H77 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay
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[PMID: 31230974] |
| MRC5 | CC50 |
>44400 nM
Compound: 39; VEL, GS-5816
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Cytotoxicity against human MRC5 cells infected with HCV genotype 1b Con-1 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay
Cytotoxicity against human MRC5 cells infected with HCV genotype 1b Con-1 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay
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[PMID: 31230974] |
| MT4 | CC50 |
>44400 nM
Compound: 39; VEL, GS-5816
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Cytotoxicity against human MT4 cells infected with HCV genotype 1a H77 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay
Cytotoxicity against human MT4 cells infected with HCV genotype 1a H77 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay
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[PMID: 31230974] |
| MT4 | CC50 |
>44400 nM
Compound: 39; VEL, GS-5816
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Cytotoxicity against human MT4 cells infected with HCV genotype 1b Con-1 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay
Cytotoxicity against human MT4 cells infected with HCV genotype 1b Con-1 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay
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[PMID: 31230974] |
| PC-3 | CC50 |
>44400 nM
Compound: 39; VEL, GS-5816
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Cytotoxicity against human PC3 cells infected with HCV genotype 1a H77 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay
Cytotoxicity against human PC3 cells infected with HCV genotype 1a H77 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay
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[PMID: 31230974] |
| PC-3 | CC50 |
>44400 nM
Compound: 39; VEL, GS-5816
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Cytotoxicity against human PC3 cells infected with HCV genotype 1b Con-1 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay
Cytotoxicity against human PC3 cells infected with HCV genotype 1b Con-1 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay
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[PMID: 31230974] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CCl4-induced non-HCV rat model[3]
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Dosage:10 mg/kg/d alone, or in combination with Sofosbuvir (20 mg/kg/d)
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Administration:p.o.
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Result:Decreased the levels of TNF-a, NF-κB and IL-6 in serum and hepatic tissues.
Inhibited hepatic stellate cells (HSCs).
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1377049-84-7
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Appearance Solid
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Masse moléculaire 883.00
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Formule C49H54N8O8
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Color White to off-white
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SMILES
O=C(N([C@H]1C)[C@@H](CC1)C2=NC3=C(C(C=C(OCC4=CC(C5=CN=C([C@H](C[C@H](COC)C6)N6C([C@@H](C7=CC=CC=C7)NC(OC)=O)=O)N5)=CC=C84)C8=C9)=C9C=C3)N2)[C@H](C(C)C)NC(OC)=O
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Synonyms
GS-5816
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (10)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. [Abstract]2021 May 29;6(1):212. PMID: 34052830 -
Hepatology
Resistance analysis of genotype 3 hepatitis C virus indicates subtypes inherently resistant to nonstructural protein 5A inhibitors. [Abstract]2019 May;69(5):1861-1872. PMID: 29425396 -
J Gastroenterol
Combinations of two drugs among NS3/4A inhibitors, NS5B inhibitors and non-selective antiviral agents are effective for hepatitis C virus with NS5A-P32 deletion in humanized-liver mice. [Abstract]2019 May;54(5):449-458. PMID: 30684016 -
Pharmaceuticals (Basel)
Evaluation of the Potency of Anti-HIV and Anti-HCV Drugs to Inhibit P-Glycoprotein Mediated Efflux of Digoxin in Caco-2 Cell Line and Human Precision-Cut Intestinal Slices. [Abstract]2022 Feb 18;15(2):242. PMID: 35215354 -
Sci Rep
Impact of novel NS5A resistance-associated substitutions of hepatitis C virus detected in treatment-experienced patients. [Abstract]2019 Apr 5;9(1):5722. PMID: 30952914 -
Viruses
Resistance Analysis of a 3-Day Monotherapy Study with Glecaprevir or Pibrentasvir in Patients with Chronic Hepatitis C Virus Genotype 1 Infection. [Abstract]2018 Aug 28;10(9). pii: E462. PMID: 30154359 -
Hepatol Res
Effects of resistance-associated variants in genotype 2 hepatitis C virus on viral replication and susceptibility to antihepatitis C virus drugs. [Abstract]2019 Nov;49(11):1275-1285. PMID: 31261439 -
J Chromatogr B Analyt Technol Biomed Life Sci
Quantification of second generation direct-acting antivirals daclatasvir, elbasvir, grazoprevir, ledipasvir, simeprevir, sofosbuvir and velpatasvir in human plasma by UPLC-MS/MS. [Abstract]2019 Mar 15:1110-1111:15-24. PMID: 30776611 -
PLoS One
The combination of the NS5A and cyclophilin inhibitors results in an additive anti-HCV inhibition in humanized mice without development of resistance. [Abstract]2021 May 20;16(5):e0251934. PMID: 34014993 -
bioRxiv
The Cyclophilin Inhibitor Rencofilstat Decreases HCV-induced Hepatocellular Carcinoma Independently of Its Antiviral Activity. [Abstract]2023 Aug 20:2023.08.19.553982. PMID: 37645728
Solvant et solubilité
DMSO : ≥ 100 mg/mL (113.25 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" 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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 mg/mL (2.83 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (2.83 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 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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (276 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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Instruction de manipulation (2659 KB)
Références
[1]. Lawitz EJ et al. Clinical Resistance to Velpatasvir (GS-5816), a Novel Pan-Genotypic Inhibitor of the Hepatitis C Virus NS5A Protein. Antimicrob Agents Chemother. 2016 Aug 22;60(9):5368-78. [Content Brief]
[2]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212. [Content Brief]
[3]. Yasmeen S, et al. An insight into the hepatoprotective role of Velpatasvir and Sofosbuvir per se and in combination against carbon tetrachloride-induced hepatic fibrosis in rats. Environ Sci Pollut Res Int. 2023 Sep;30(42):95660-95672. [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 |
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| DMSO | 1 mM | 1.1325 mL | 5.6625 mL | 11.3250 mL | 28.3126 mL |
| 5 mM | 0.2265 mL | 1.1325 mL | 2.2650 mL | 5.6625 mL | |
| 10 mM | 0.1133 mL | 0.5663 mL | 1.1325 mL | 2.8313 mL | |
| 15 mM | 0.0755 mL | 0.3775 mL | 0.7550 mL | 1.8875 mL | |
| 20 mM | 0.0566 mL | 0.2831 mL | 0.5663 mL | 1.4156 mL | |
| 25 mM | 0.0453 mL | 0.2265 mL | 0.4530 mL | 1.1325 mL | |
| 30 mM | 0.0378 mL | 0.1888 mL | 0.3775 mL | 0.9438 mL | |
| 40 mM | 0.0283 mL | 0.1416 mL | 0.2831 mL | 0.7078 mL | |
| 50 mM | 0.0227 mL | 0.1133 mL | 0.2265 mL | 0.5663 mL | |
| 60 mM | 0.0189 mL | 0.0944 mL | 0.1888 mL | 0.4719 mL | |
| 80 mM | 0.0142 mL | 0.0708 mL | 0.1416 mL | 0.3539 mL | |
| 100 mM | 0.0113 mL | 0.0566 mL | 0.1133 mL | 0.2831 mL |
Velpatasvir Related Classifications
HY-12530 Related Classifications
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