| Bioactivity | Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import[1][2][3][4]. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19[5]. | ||||||||||||
| Invitro | 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[1]. 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[1].Ivermectin (MK-933) activates glutamate-gated chloride channels in the nerves and muscles of the parasite, leading to membrane hyperpolarization and muscle paralysis[2].Ivermectin (MK-933) strongly inhibits the binding of Impα/β1 to NS5 (IC50=17 μM), but not of Impβ1 alone to NS5[3].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[3]. | ||||||||||||
| Name | Ivermectin | ||||||||||||
| CAS | 70288-86-7 | ||||||||||||
| Formula | C48H74O14 | ||||||||||||
| Molar Mass | 875.09 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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