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| | Olgotrelvir Basic information |
| Product Name: | Olgotrelvir | | Synonyms: | Olgotrelvir;3-Pyrrolidinepropaney, α-hydroxy-β-[[(2S)-2-[(1H-indol-2-ylcarbonyl)amino]-4-methyl-1-oxopentyl]amino]-2-oxo-, (βS,3S)-;(2S)-2-[(S)-2-(1H-Indole-2-carboxamido)-4-methylpentanamido]-1-hydroxy-3-[(S)-2-oxo-3-pyrrolidinyl]propane-1-sulfonic Acid | | CAS: | 2763596-71-8 | | MF: | C22H30N4O7S | | MW: | 494.56 | | EINECS: | | | Product Categories: | | | Mol File: | 2763596-71-8.mol |  |
| | Olgotrelvir Chemical Properties |
| density | 1.393±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | | pka | 0.654±0.50(predicted) |
| | Olgotrelvir Usage And Synthesis |
| Uses | 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[1][2]. | | in vivo | Olgotrelvir (400-1000 mg/kg; p.o.; twice a day immediately after viral inoculation) has antiviral activity and reduces lung pathology in K18-hACE2 transgenic mice[2].
| 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] | | Dosage: | 400, 500, 1000 mg/kg | | Administration: | Oral gavage (p.o.); twice a day immediately after SARS-CoV-2 WA-1 strain inoculation | | 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.
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| | References | [1] Sorrento Announces the Full Enrollment of the Pivotal Phase 3 Trial with Olgotrelvir (OVYDSOTM) (STI-1558), a Second Generation Oral Mpro Inhibitor, as a Standalone Treatment for COVID-19. |
| | Olgotrelvir Preparation Products And Raw materials |
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