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製品番号: HY-175461

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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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 3105041-48-0
分子式: C₁₉H₂₃N₇O₂
分子量:381.43

保管条件:

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

Data Sheet (276 KB)

AVI-4206 構造式

CAS 番号: 3105041-48-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性

製品説明

体外実験

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.

体内実験

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.

化学情報

CAS 番号 3105041-48-0
分子量 381.43
分子式 C₁₉H₂₃N₇O₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (276 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Suryawanshi RK, et al. The Mac1 ADP-ribosylhydrolase is a Therapeutic Target for SARS-CoV-2. bioRxiv [Preprint]. 2024 Aug 29:2024.08.08.606661. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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