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].

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

875.09

C₉₅H₁₄₆O₂₈

70288-86-7

伊维菌素

Room temperature in continental US; may vary elsewhere.

DMSO : 250 mg/mL (285.68 mM; Need ultrasonic)

H₂O : 0.1 mg/mL (0.11 mM; Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (2.86 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (2.86 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.08 mg/mL (2.38 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (2.38 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Khakh BS, et al. Allosteric control of gating and kinetics at P2X(4) receptor channels. J Neurosci. 1999 Sep 1;19(17):7289-99.

  [2]. Priel A, et al. Mechanism of ivermectin facilitation of human P2X4 receptor channels. J Gen Physiol. 2004 Mar;123(3):281-93.

  [3]. Wagstaff KM, et al. Ivermectin is a specific inhibitor of importin α/β-mediated nuclear import able to inhibit replication of HIV-1 and dengue virus. Biochem J. 2012 May 1;443(3):851-6.

  [4]. Raza S, et al. Ivermectin Inhibits Bovine Herpesvirus 1 DNA Polymerase Nuclear Import and Interferes with Viral Replication. Microorganisms. 2020 Mar 13;8(3). pii: E409.

  [5]. Khan Sharun, et al. Ivermectin, a New Candidate Therapeutic Against SARS-CoV-2/COVID-19. Ann Clin Microbiol Antimicrob. 2020 May 30;19(1):23.