An inhibitor of kallikrein and TMPRSS2
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Avoralstat

Item No. 35610

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[2-[[[4-(aminoiminomethyl)phenyl]amino]carbonyl]-4-ethenyl-5-methoxyphenyl]-6-[[(cyclopropylmethyl)amino]carbonyl]-2-pyridinecarboxylic acid
CAS Number
918407-35-9
Synonyms
  • BCX 4161
Molecular Formula
C28H27N5O5
Formula Weight
513.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 50 mg/ml
λmax
218, 246, 286 nm
SMILES
O=C(C1=C(C2=C(C(NC3=CC=C(C(N)=N)C=C3)=O)C=C(C=C)C(OC)=C2)C=CC(C(NCC4CC4)=O)=N1)O
InChi Code
InChI=1S/C28H27N5O5/c1-3-16-12-21(26(34)32-18-8-6-17(7-9-18)25(29)30)20(13-23(16)38-2)19-10-11-22(33-24(19)28(36)37)27(35)31-14-15-4-5-15/h3,6-13,15H,1,4-5,14H2,2H3,(H3,29,30)(H,31,35)(H,32,34)(H,36,37)
InChi Key
TUWMKPVJGGWGNL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Cayman Chemical
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    Product Description

    Avoralstat is an inhibitor of kallikrein, a serine protease involved in the contact activation system.1 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.2,3 It inhibits SARS-CoV-2 pseudovirus entry into Calu-3 2B4 cells (EC50 = 0.7 µM).2 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cornpropst, M., Collis, P., Collier, J., et al. Safety, pharmacokinetics, and pharmacodynamics of avoralstat, an oral plasma kallikrein inhibitor: Phase 1 study. Allergy 71(12), 1676-1683 (2016).

    2. Sun, Y.J., Velez, G., Parsons, D.E., et al. Structure-based phylogeny identifies avoralstat as a TMPRSS2 inhibitor that prevents SARS-CoV-2 infection in mice. J. Clin. Invest. 131(10), e147973 (2021).

    3. Hu, X., Shrimp, J.H., Guo, H., et al. Discovery of TMPRSS2 inhibitors from virtual screening as a potential treatment of COVID-19. ACS Pharmacol. Transl. Sci. 4(3), 1124-1135 (2021).