Olgotrelvir
Olgotrelvir (STI-1558) is an orally active dual inhibitor of coronavirus main protease (Mpro) and human cell cathepsin (Cathepsin L). Olgotrelvir is readily converted to its active form, AC1115, in full blood and/or plasma. Olgotrelvir can effectively inhibit both SARS-CoV-2 replication and entry into host cells.
The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Olgotrelvir sodium) that retains the same biological activity.
For research use only. We do not sell to patients.
- CAS No.: 2763596-71-8
- Formula: C22H30N4O7S
- Molecular Weight:494.56
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
In Vitro
Olgotrelvir (0-100 μM; refresh every other day for 3 to 5 days) displays antiviral activity against all tested SARS-CoV-2 VOCs, including WA-1, Alpha, Beta, Delta, Lambda, and Gamma variants with average EC50 values of 0.28 to 4.26 μM in vero E6 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | AUC | T1/2 | Plasma Concentration | Tmax | Bioavailability |
|---|---|---|---|---|---|---|---|
| Cynomolgus Monkey | 84 mg/kg | p.o. | 90900 ng·h/mL | 4.84 h | 18800 ng/mL | 2.7 h | 48.3 % |
| Dog | 12.5 mg/kg | p.o. | 15200 ng·h/mL | 4.01 h | 3600 ng/mL | 2.0 h | 83.1 % |
| Dog | 25 mg/kg | p.o. | 30500 ng·h/mL | 3.76 h | 7080 ng/mL | 1.5 h | 83.5 % |
| Dog | 50 mg/kg | p.o. | 61800 ng·h/mL | 3.51 h | 13200 ng/mL | 2.0 h | 84.7 % |
| Mice | 300 mg/kg | p.o. | 8030 ng·h/mL | 1.58 h | 7290 ng/mL | 0.25 h | 5.06 % |
| Mice | 500 mg/kg | p.o. | 12400 ng·h/mL | 1.9 h | 10600 ng/mL | 0.25 h | 4.69 % |
| Rat | 100 mg/kg | p.o. | 2000 ng·h/mL | 1.48 h | 1200 ng/mL | 0.17 h | 2.94 % |
| Rat | 200 mg/kg | p.o. | 3580 ng·h/mL | 1.84 h | 2650 ng/mL | 0.083 h | 2.62 % |
| Rat | 500 mg/kg | p.o. | 8050 ng·h/mL | 2.03 h | 6460 ng/mL | 0.083 h | 2.36 % |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:K18-hACE2 transgenic mice (express human ACE2 in the lung epithelia, including airway epithelia, under the control of the human keratin 18 promoter)[2]
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Dosage:400, 500, 1000 mg/kg
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Administration:Oral gavage (p.o.); twice a day immediately after SARS-CoV-2 WA-1 strain inoculation
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Result:Prevented weight loss.
On day 5 post infection, virus was below the detectable level in the lungs.
Pathological changes caused by SARS-CoV-2 infection were relieved.
At a dose of 1000 mg/kg at the 12th hour post-infection resulted in significant reduction of viral RNA shedding and prevention of the body weight loss.
Blocked pro-inflammatory cytokine (IL-6, TNF-α, GM-CSF) release at 400 mg/kg dosage.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2763596-71-8
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Molecular Weight 494.56
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Formula C22H30N4O7S
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SMILES
O=C(NCC1)[C@@H]1C[C@@H](C(O)S(=O)(O)=O)NC([C@H](CC(C)C)NC(C2=CC3=CC=CC=C3N2)=O)=O
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Synonyms
STI-1558
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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)
Olgotrelvir Related Classifications
HY-156655 Related Classifications
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