2. Anti-infection
  3. Virus Protease SARS-CoV
  4. 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).

For research use only. We do not sell to patients.

MR1-114

MR1-114 Chemical Structure

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MR1-114 Related Antibodies

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Description

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)[1].

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.

MR1-114 Related Antibodies
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

MR1-114 (100-150 mg/kg; p.o.; twice daily; for 5 consecutive days) prevents disease-associated body weight loss and reduces pulmonary viral replication levels in K18-ACE2 mice infected with SARS-CoV-2 WA1[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: B6.Cg-Tg(K18-ACE2)2Prlmn/J (female, 6−8 weeks of age, SARS-CoV-2 WA1 intranasal challenge)[1]
Dosage: 100 mg/kg; 150 mg/kg
Administration: p.o.; twice daily; 5 days
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).
Molecular Weight

521.66

Formula

C31H35N7O
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MR1-114 Related Classifications

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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.

Keywords:

MR1-114Virus ProteaseSARS-CoVSARS coronavirusK18-ACE2 miceA549-hACE2 cellsSARS-CoV-2 papain-like proteaseVal70Ub pocketBL2 grooveOmicron BA.5PLproDeltacovid-19SARS-CoV-2 variantsInhibitorinhibitorinhibit

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