| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
AVI-4206 (0.1-1,000,000 nM) inhibits the catalytic activity of Mac1, with an IC50 value of 64 nM in the ADP-ribosylated PARP10 and NudT5/AMP-Glo conjugate assay[1]. AVI-4206 (10 μM) binds efficiently and selectively to Mac1 in A549 cells[1]. AVI-4206 (0.01-10,000 nM) has limited inhibitory effect on SARS-CoV-2 infection in Vero-TMPRSS2 or A549-ACE2h cells[1]. AVI-4206 (0.16-100 μM, 24-72 h) reduces viral particle yield after infection with Mac1-deficient virus (WA1 N40D mutant)[1].
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|---|---|
| ln Vivo |
AVI-4206 (100 mg/kg, intraperitoneal injection, twice daily for 7 days) was effective in the K18-hACE2 mouse SARS-CoV-2 infection model [1].
|
| Animal Protocol |
Animal/Disease Models:Female K18-hACE2 mice were infected with the WA1 N40D mutant strain lacking Mac1 catalytic activity [1].
Doses: 100 mg/kg Route of Administration: Intraperitoneal injection, twice daily for 7 days (until day 5 post-infection). Experimental Results: Weight loss occurred on day 4 post-infection, but the average weight loss was reduced by approximately 5-10% compared to the corresponding vector control group on days 5-7 post-infection. It reduced disease severity and prevented death in the K18-hACE2 model. It accelerated the clearance of viral load from the lungs. It increased the levels of antiviral cytokines IP-10, IL-2, IL-6, and TNF-α in lung tissue. |
| References |
| Molecular Formula |
C19H23N7O2
|
|---|---|
| Molecular Weight |
381.43
|
| CAS # |
3105041-48-0
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(NCC)NC1=CC=CC2=C1NC3=NC=NC(NN4C(C)(C)CCC4=O)=C32
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6217 mL | 13.1086 mL | 26.2171 mL | |
| 5 mM | 0.5243 mL | 2.6217 mL | 5.2434 mL | |
| 10 mM | 0.2622 mL | 1.3109 mL | 2.6217 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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