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AVI-4206 is a selective Mac1 inhibitor with an IC50 of 64 nM for inhibiting Mac1's catalytic activity. It effectively reduces SARS-CoV-2 viral replication, restores interferon response, and demonstrates survival benefits in animal models infected with SARS-CoV-2. AVI-4206 is applicable for research related to SARS-CoV-2 infections.
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| Description | AVI-4206 is a selective Mac1 inhibitor with an IC50 of 64 nM for inhibiting Mac1's catalytic activity. It effectively reduces SARS-CoV-2 viral replication, restores interferon response, and demonstrates survival benefits in animal models infected with SARS-CoV-2. AVI-4206 is applicable for research related to SARS-CoV-2 infections. |
| In vitro | AVI-4206 inhibits the catalytic activity of Mac1 in PARP10 self-ADP-ribosylation and coupled NudT5/AMP-Glo assays, with an IC50 of 64 nM within concentrations of 0.1-1000000 nM. It binds with high efficiency and selectivity to Mac1 in A549 cells at 10 μM. However, AVI-4206 shows limited efficacy in SARS-CoV-2 infected Vero-TMPRSS2 or A549-ACE2h cells at concentrations ranging from 0.01-10000 nM. In addition, AVI-4206 at concentrations of 0.16-100 μM over 24-72 hours reduces viral particle production following infection by a Mac1 deletion virus (WA1 N40D mutant). |
| In vivo | AVI-4206, administered intraperitoneally at a dose of 100 mg/kg twice daily for 7 consecutive days, demonstrates efficacy in the K18-hACE2 mouse model of SARS-CoV-2 infection. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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