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ML2006a4 is an orally active inhibitor for SARS-CoV-2 main protease (Mpro) with IC50 in picomolare value. ML2006a4 is cell permeable and antiviral active, that inhibits replication in SARS-CoV-2 in cells Huh7.5.1-ACE2-TMPRSS2 (Huh7.5.1++) in picomolare level[1] | [in vivo]
ML2006a4 (20 mg/kg, i.v.) reveals a pharmacokinetic profils with an oral bioavailability of 27% (40 mg/kg, p.o.) and a plasma clearance rate Cpl of 39 mL/min/kg and Volume of distribution at steady state Vss 0.66 L/kg[1].
ML2006a4 (40 mg/kg, p.o., twice a day for 4 days) ameliorates the SARS-CoV-2 infection, exhibits viral inhibitory and lung protective efficacy in BALB/c mice without significant toxicity[1]. | Animal Model: | SARS-CoV-2 MA10 infected BALB/c mice[1] | | Dosage: | 40 mg/kg | | Administration: | p.o., twice a day for 4 days | | Result: | Reduced inflammation and respioratory epithelial injury, improved epithelial regeneration and the survival rates with minimal weight loss. |
| [References]
[1] Westberg M, et al., An orally bioavailable SARS-CoV-2 main protease inhibitor exhibits improved affinity and reduced sensitivity to mutations. Sci Transl Med. 2024 Mar 13;16(738):eadi0979. DOI:10.1126/scitranslmed.adi0979 |
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