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.
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- CAS No.: 2763596-71-8
- 화학식: C22H30N4O7S
- 분자량:494.56
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보관:
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
- 순도&문서
- References
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Help & FAQs
All Cathepsin Isoforms
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Biological Activity
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.
| 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 % |
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2763596-71-8
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분자량 494.56
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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