Narlaprevir
Based on 5 publication(s) in Google Scholar
Narlaprevir (SCH 900518) is a selective and orally bioavailable NS3 protease inhibitor with a Ki value of 6 nM and an EC90 value of 40 nM. Narlaprevir also inhibits the HCV nonstructural protein 3 serine protease. Narlaprevir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 2.3 μM.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 95.88%
- CAS No.: 865466-24-6
- Formule: C36H61N5O7S
- Masse moléculaire:707.96
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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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Publications Citing Use of MedChemExpress (MCE) Narlaprevir
More
Activité biologique
Ki: 6 nM (NS3 protease) [1]
EC90: 40 nM (NS3 protease) [1]
Ki: 7 nM (ketoamide) [2]
EC90: 40 nM (replicon RNA) [2]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | CC50 |
>25 μM
Compound: SCH-900518
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Cytotoxicity against human HuH7 cells by MTS assay
Cytotoxicity against human HuH7 cells by MTS assay
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[PMID: 20308381] |
| Vero C1008 | EC50 |
7.7 μM
Compound: Narlaprevir
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Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 expressing recombinant TMPRSS2 assessed as reduction in viral growth
Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 expressing recombinant TMPRSS2 assessed as reduction in viral growth
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[PMID: 37659195] |
Narlaprevir (SCH 900518) exhibits middle oral bioavailability (rat 46%, dog 29%, monkey 46 %) following oral administration (rat 10 mg/kg, dog 3 mg/kg, monkey 3 mg/kg )[1].
Narlaprevir (SCH 900518) exhibits moderate half-lives (rat 4.8 and dog 2 h) following intravenous administration (rat 4 and dog 1 mg/kg)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:rats, dogs, monkeys[1]
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Dosage:Rat PO/IV 10/4 mg/kg; dog PO/IV 3/1 mg/kg; monkey PO 3 mg/kg
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Administration:Intravenous (i.v.) or oral gavage
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Result:T1/2s of 4.8 and 2 h for rats and dogs, respectively.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 865466-24-6
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Appearance Solid
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Masse moléculaire 707.96
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Formule C36H61N5O7S
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Color White to off-white
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SMILES
O=S(CC1(NC(N[C@H](C(N2[C@@H]([C@@]3([H])C(C)([C@]3(C2)[H])C)C(N[C@H](C(C(NC4CC4)=O)=O)CCCC)=O)=O)C(C)(C)C)=O)CCCCC1)(C(C)(C)C)=O
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Synonyms
SCH 900518
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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 (5)
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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 -
Signal Transduct Target Ther
Structural basis for the inhibition of the SARS-CoV-2 main protease by the anti-HCV drug narlaprevir. [Abstract]2021 Feb 4;6(1):51. PMID: 33542181 -
Cell Rep
Hepatitis C virus drugs that inhibit SARS-CoV-2 papain-like protease synergize with remdesivir to suppress viral replication in cell culture. [Abstract]2021 May 18;35(7):109133. PMID: 33984267 -
Sci Rep
Hepatitis C virus NS3/4A inhibitors and other drug-like compounds as covalent binders of SARS-CoV-2 main protease. [Abstract]2022 Jul 16;12(1):12197. PMID: 35842458 -
SLAS Discov
2025 Mar:31:100211. PMID: 39824441
Solvant et solubilité
DMSO : ≥ 50 mg/mL (70.63 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" 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 (3.53 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.
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 (281 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Ashok Arasappan, et al. Discovery of Narlaprevir (SCH 900518): A Potent, Second Generation HCV NS3 Serine Protease Inhibitor. ACS Med Chem Lett. 2010 Feb 15;1(2):64-9. [Content Brief]
[2]. X Tong, et al. Preclinical characterization of the antiviral activity of SCH 900518 (narlaprevir), a novel mechanism-based inhibitor of hepatitis C virus NS3 protease. Antimicrob Agents Chemother. 2010 Jun;54(6):2365-70. [Content Brief]
[3]. 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]
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 | 1.4125 mL | 7.0625 mL | 14.1251 mL | 35.3127 mL |
| 5 mM | 0.2825 mL | 1.4125 mL | 2.8250 mL | 7.0625 mL | |
| 10 mM | 0.1413 mL | 0.7063 mL | 1.4125 mL | 3.5313 mL | |
| 15 mM | 0.0942 mL | 0.4708 mL | 0.9417 mL | 2.3542 mL | |
| 20 mM | 0.0706 mL | 0.3531 mL | 0.7063 mL | 1.7656 mL | |
| 25 mM | 0.0565 mL | 0.2825 mL | 0.5650 mL | 1.4125 mL | |
| 30 mM | 0.0471 mL | 0.2354 mL | 0.4708 mL | 1.1771 mL | |
| 40 mM | 0.0353 mL | 0.1766 mL | 0.3531 mL | 0.8828 mL | |
| 50 mM | 0.0283 mL | 0.1413 mL | 0.2825 mL | 0.7063 mL | |
| 60 mM | 0.0235 mL | 0.1177 mL | 0.2354 mL | 0.5885 mL |
Narlaprevir Related Classifications
HY-10300 Related Classifications
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