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Ivermectin

CAS No. : 70288-86-7

MCE 国际站：Ivermectin

产品活性：Ivermectin (MK-933) 是一种广谱的抗寄生虫活性分子。Ivermectin (MK-933) 是一种特异性的 Impα/β1 介导的核导入抑制剂，对 HIV-1 和登革热病毒都具有很强的抗病毒活性。Ivermectin (MK-933) 也是 P2X₄ 和 α7 nAChRs 的正异构效应物。Ivermectin 还可抑制牛疱疹病毒 1 (BoHV-1) 复制并抑制 BoHV-1 DNA 聚合酶的核输入。Ivermectin 是应用于抗 SARS-CoV-2/COVID-19 的候选活性分子。

研究领域：Anti-infection  |  Autophagy

作用靶点：Parasite  |  HIV  |  Mitophagy  |  HSV  |  SARS-CoV  |  Antibiotic  |  Autophagy  |  Bacterial

结构分类：抗生素  |  疾病研究  |  抗病毒  |  抗生素  |  疾病研究  |  抗虫  |  抗生素  |  大环内脂类  |  结构分类

In Vitro: In the submicromolar range (EC₅₀=250 nM) the action of Ivermectin (MK-933) is rapid and reversible, resulting in increased amplitude and slowed deactivation of P2X₄ channel currents evoked by ATP.
Ivermectin (MK-933) markedly increases the potency of ATP and that of the normally low-potency agonist a,b-methylene-ATP in a use- and voltage-independent manner without changing the ion selectivity of P2X₄ channels.
Ivermectin (MK-933) activates glutamate-gated chloride channels in the nerves and muscles of the parasite, leading to membrane hyperpolarization and muscle paralysis.
Ivermectin (MK-933) strongly inhibits the binding of Impα/β1 to NS5 (IC₅₀=17 μM), but not of Impβ1 alone to NS5.
Ivermectin (MK-933) has potent antiviral activity towards both HIV-1 and dengue virus, both of which are strongly reliant on importin α/β nuclear import, with respect to the HIV-1 integrase and NS5 (non-structural protein 5) polymerase proteins respectively.

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