MR1-114
MR1-114 is an orally active SARS-CoV-2 papain-like protease (PLpro) inhibitor with an IC50 of 0.037 μM. As a broad-spectrum inhibitor, MR1-114 maintains submicromolar activity against SARS-CoV-2 Delta, Omicron B.1.1.529 and Omicron BA.5 variants, with EC50 values of 0.18 μM, 0.39 μM and 0.20 μM, respectively. MR1-114 can be used for the research of coronavirus disease 2019 (SARS-CoV-2 infection).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C31H35N7O
- Masse moléculaire:521.66
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
MR1-114 potently inhibits purified recombinant SARS-CoV-2 PLpro with an IC50 value of 0.037 μM[1].
MR1-114 (48 h) exhibits low cytotoxicity in A549-hACE2 cells, with a CC50 of 34.54 μM[1].
MR1-114 (1-10 μM; 1 h) potently inhibits the replication of SARS-CoV-2 WA1 in A549-hACE2 cells, reducing viral load by 1.54 log at 1 μM and by 6.41 log at 10 μM[1].
MR1-114 (2 h) acts as a broad-spectrum inhibitor that retains submicromolar activity against SARS-CoV-2 Delta, Omicron B.1.1.529 and Omicron BA.5 variants in A549-hACE2 cells, with EC50 values of 0.18 μM, 0.39 μM and 0.20 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 | AUCinf | CL_obs | Vss_obs | Bioavailability |
|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 2.11 h | 6091 (plasma) ng·h/mL | / | / | 60.2 % |
| Mice[1] | 1 mg/kg | i.v. | 1.80 h | 1012 (plasma) ng·h/mL | 16.7 mL/min/kg | 2.33 L/kg | / |
| Rat[1] | 10 mg/kg | p.o. | 2.78 h | 10954 (plasma) ng·h/mL | / | / | 71.2 % |
| Rat[1] | 1 mg/kg | i.v. | 3.00 h | 1538 (plasma) ng·h/mL | 11.0 (plasma) mL/min/kg | 2.40 L/kg | / |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:B6.Cg-Tg(K18-ACE2)2Prlmn/J (female, 6−8 weeks of age, SARS-CoV-2 WA1 intranasal challenge)[1]
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Dosage:100 mg/kg; 150 mg/kg
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Administration:p.o.; twice daily; 5 days
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Result:Maintained body weight percentages comparable to mock-infected and nirmatrelvir-treated groups, preventing disease-associated weight loss.
Produced a statistically significant ~1 log decrease in lung viral titers relative to vehicle control at 150 mg/kg, comparable to Nirmatrelvir (1000 mg/kg, twice daily).
Chemical Information
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Masse moléculaire 521.66
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Formule C31H35N7O
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SMILES
CC1=CC=C(C=C1C(N[C@@H](C2=CC(C#CC3=CN(N=C3)C)=CC(C4=CN(N=C4)C)=C2)C)=O)N5CCN(CC5)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MR1-114 Related Classifications
HY-182894 Related Classifications
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