Formulation: A solid
Formal Name: 3-[2-[[[4-(aminoiminomethyl)phenyl]amino]carbonyl]-4-ethenyl-5-methoxyphenyl]-6-[[(cyclopropylmethyl)amino]carbonyl]-2-pyridinecarboxylic acid
Purity: ≥98%
Formula Markup: C28H27N5O5
Formula Weight: 513,6
Shelf life (days): 1460
CAS Number: 918407-35-9
Notes: Avoralstat is an inhibitor of kallikrein, a serine protease involved in the contact activation system.{65255} It inhibits kallikrein activity in isolated human plasma (EC50s = 1.14-11.1 nM). Avoralstat also inhibits transmembrane serine protease 2 (TMPRSS2; IC50 = 2.73 nM), a serine protease required for entry of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) into host cells.{65256,65257} It inhibits SARS-CoV-2 pseudovirus entry into Calu-3 2B4 cells (EC50 = 0.7 µM).{65256} Avoralstat (30 mg/kg) reduces or prevents the accumulation of lung viral titers in mouse models of SARS-CoV-2 infection or prophylaxis, respectively, using Ad5-hACE2 mice that are sensitive to SARS-CoV-2 infection.
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