1. Anti-infection
  2. SARS-CoV
  3. AVI-4206

AVI-4206 is a selective Mac1 inhibitor with an lC50 of 64 nM. AVI-4206 reduces viral replication, restores an interferon response, and leads to a survival benefit in an animal model of SARS-CoV-2 infection. AVI-4206 can be used the study of SARS-CoV-2 infection.

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AVI-4206

AVI-4206 Chemical Structure

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Description

AVI-4206 is a selective Mac1 inhibitor with an lC50 of 64 nM. AVI-4206 reduces viral replication, restores an interferon response, and leads to a survival benefit in an animal model of SARS-CoV-2 infection. AVI-4206 can be used the study of SARS-CoV-2 infection[1].

In Vitro

AVI-4206 (0.1-1000000 nM) inhibits the catalytic activity of Mac1 with an IC50 of 64 nM in the auto ADP-ribosylated PARP10 and a coupled NudT5/AMP-Glo assay[1].
AVI-4206 (10 μM) engages Mac1 with high potency and selectivity in A549 cells[1].
AVI-4206 (0.01-10000 nM) shows limited efficacy against SARS-CoV-2 infection in Vero-TMPRSS2 or A549-ACE2h cells[1].
AVI-4206 (0.16-100 μM, 24-72 h) reduces viral particle production after Mac1 deficient virus (WA1 N40D mutant) infection[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

AVI-4206 (100 mg/kg, i.p., twice daily, 7 days) is effective in K18-hACE2 mouse model of SARS-CoV-2 infection[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female K18-hACE2 mice were infected with WA1 N40D mutant, which lacks Mac1 catalytic activity[1]
Dosage: 100 mg/kg
Administration: i.p., twice daily for 7 days (until 5 days post-infection)
Result: Showed weight loss at 4 days post-infection, but the extent of weight loss was about 5-10% lower on average at days 5-7 post-infection compared with respective vehicle-treated groups.
Reduced disease severity and prevent death in the K18-hACE2 model.
Showed the faster clearance of viral load in the lungs.
Increased the levels of antiviral cytokines IP-10, IL-2, IL-6, and TNF-α in lung tissue.
Molecular Weight

381.43

Formula

C19H23N7O2

SMILES

O=C(NCC)NC1=CC=CC2=C1NC3=NC=NC(NN4C(C)(C)CCC4=O)=C32

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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AVI-4206 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
AVI-4206
Cat. No.:
HY-175461
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