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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
| 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 |
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.
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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