MERS-CoV-IN-4
MERS-CoV-IN-4 is an orally active antiviral inhibitor targeting the MERS-CoV spike (S) protein, with an IC50 of 0.009 μM in Huh-7 cells, and Kd values of 7.72 μM for the full-length S protein and 5.09 μM for S-RBD. MERS-CoV-IN-4 inhibits viral entry, and suppresses MERS-CoV pseudoviruses and live viruses in vitro. MERS-CoV-IN-4 reduces pulmonary viral loads in hDPP4 transgenic mice. MERS-CoV-IN-4 can be used for research on Middle East respiratory syndrome coronavirus infection.
For research use only. We do not sell to patients.
- CAS No.: 2740494-38-4
- Formula: C19H22N4S
- Molecular Weight:338.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
MERS-CoV-IN-4 (Compound 22) potently inhibits MERS-CoV pseudovirus in Huh-7 cells, with an IC50 of 0.009 μM and a selectivity index of approximately 1494[1].
MERS-CoV-IN-4 inhibits live MERS-CoV (EMC/2012) in Vero-81 cells, with an EC50 of 2.282 μM and a selectivity index of approximately 5.67[1].
MERS-CoV-IN-4 (5-10 μM; 3 h pre-treatment) acts on the early stage of the MERS-CoV life cycle in Vero-81 cells, with an inhibition rate of 30% at 5 μM and over 50% at 10 μM[1].
MERS-CoV-IN-4 (0.24-15.63 μM; 60 s contact, 60 s dissociation) directly binds to purified full-length MERS-CoV S protein (KD = 7.72 μM) and MERS-CoV S-RBD (KD = 5.09 μM) in cell-free SPR assays[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUClast | AUCINF_obs | MRTINF_obs |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 40 mg/kg | p.o. | 12.7 h | 4.17 h | 333 ng/mL | 3461 ng·h/mL | 4665 ng·h/mL | 18.8 h |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:hDPP4-KI mice (male, 7-8 weeks old, intranasal inoculation with MERS-CoV EMC/2012 strain)[1]
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Dosage:50 mg/kg; 100 mg/kg
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Administration:i.g.; twice daily; 3-7 consecutive days
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Result:Reduced lung viral load by ~1-log10 and extended median survival time to 6 days (compared to 5 days in vehicle controls).
Reduced lung viral load by ~1-log10 and extended median survival time to 7 days (compared to 5 days in vehicle controls).
Chemical Information
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CAS No. 2740494-38-4
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Molecular Weight 338.47
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Formula C19H22N4S
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SMILES
C12=CC=CC=C1SC(C3=CC=C(NCCN4CCNCC4)C=C3)=N2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MERS-CoV-IN-4 Related Classifications
HY-184669 Related Classifications
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