1. Anti-infection Others
  2. Influenza Virus Drug Derivative
  3. Antiviral agent 80

Antiviral agent 80 是 Zanamivir (HY-13210)-Amantadine (HY-13317) 偶联物,是流感病毒 M2 离子通道/神经氨酸酶 (NA) 的双重抑制剂。Antiviral agent 80 对野生型及耐药性流感神经氨酸酶突变体均表现出强效抑制活性,其 IC50 值范围为 1.50 nM 至 120.4 nM。Antiviral agent 80 可用于流感的相关研究。

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Antiviral agent 80

Antiviral agent 80 Chemical Structure

CAS No. : 3110745-57-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Antiviral agent 80 is a conjugate of Zanamivir (HY-13210) and Amantadine (HY-13317), acting as a dual inhibitor of influenza virus M2 ion channel/neuraminidase (NA). Antiviral agent 80 exhibits potent inhibitory activity against both wild-type and drug-resistant influenza neuraminidase mutants, with an IC50 value range of 1.50 nM to 120.4 nM. Antiviral agent 80 can be used in influenza-related research[1].

体外研究
(In Vitro)

Antiviral agent 80 (Compound 7j) 对野生型及耐药性流感神经氨酸酶 (NA) 突变体均表现出强效抑制活性,其 IC50 值范围为 1.50 nM 至 120.4 nM,其中对 N9、N1、N1 (H275Y) 的 IC50 分别为 1.5、1.69 和 2.05 nM[1]
Antiviral agent 80 可保护 MDCK 细胞免受甲型流感病毒诱导的细胞病变效应,其 EC50 值范围为 11.13 nM 至 12.55 nM,CC50 大于 200 μM,表明其具有高选择性[1]
Antiviral agent 80 (5 μM; 24 h) 可在转染 NA 质粒的 HEK293T 细胞中诱导蛋白酶体依赖的 NA 降解,降解率约达 95%;且不会上调 BEAS-2B、HEK293T 或 A549 细胞中的自噬标志物[1]
Antiviral agent 80 可高效穿过细胞膜并在 MDCK 细胞中蓄积,在 100 μM 和 25 μM 的预处理浓度下细胞内滞留率分别为 88.8% 和 19.1%;清洗细胞外的化合物后,其针对 A/WSN/1933 的 EC50 仅从 11.13 nM 小幅上升至 48.0 nM,表明该化合物具有较强的细胞内抗病毒活性[1]
Antiviral agent 80 可在 MDCK 细胞中抑制甲型流感病毒生命周期的多个阶段,这一点可通过 M1 蛋白水平的降低得到证明[1]

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

Western Blot Analysis[1]

Cell Line: HEK293T cells transfected with NA plasmids; BEAS-2B, HEK293T, A549 cells
Concentration: 5 μM (NA degradation); 5 μM (MG-132, proteasome inhibitor); 100 μM (chloroquine, lysosomal inhibitor)
Incubation Time: 24 h (NA degradation)
Result: Reduced NA protein levels in a dose- and time-dependent manner in HEK293T cells transfected with NA plasmids, with ~95% degradation observed after 24 h treatment with 5 μM.
Blocked NA degradation in the presence of 5 μM proteasome inhibitor MG-132 but not 100 μM lysosomal inhibitor chloroquine.
Did not upregulate autophagy markers (LC3-II, ATG5, ATG7) in BEAS-2B, HEK293T, or A549 cells, unlike Amantadine.
分子量

580.63

Formula

C26H40N6O9

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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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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Antiviral agent 80
目录号:
HY-181885
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