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Avoralstat

Chemical Structure : Avoralstat

CAS No.: 918407-35-9

Avoralstat (BCX4161, BCX-4161)

Catalog No.: PC-25823Not For Human Use, Lab Use Only.

Avoralstat (BCX4161) is a potent and orally active plasma kallikrein inhibitor, also is a potent, selective Transmembrane protease, serine 2 (TMPRSS2) inhibitor (IC50=2.73 nM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Avoralstat (BCX4161) is a potent and orally active plasma kallikrein inhibitor, also is a potent, selective Transmembrane protease, serine 2 (TMPRSS2) inhibitor (IC50=2.73 nM).
Avoralstat is 18-fold more selective toward TMPRSS2 than other S1 proteases.
Avoralstat inhibits viral entry directed by SARS-CoV-2 spike proteins.
Avoralstat inhibits SARS-CoV-2 pseudovirus entry with EC50 of 2.8 uM.
Avoralstat (30 mg/kg i.p. injection) reduces SARS-CoV-2 infection in mice.

Physicochemical Properties

M.Wt 513.55
Formula C28H27N5O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-(2-((4-Carbamimidoylphenyl)carbamoyl)-5-methoxy-4-vinylphenyl)-6-((cyclopropylmethyl)carbamoyl)picolinic acid

References

1. Riedl MA, et al. Allergy. 2018 Sep;73(9):1871-1880.

2. Sun YJ, et al. J Clin Invest. 2021 May 17;131(10):e147973.

3. Zhang J, et al. Med Chem. 2006 Nov;2(6):545-53.

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