loadingProduct Data?SheetIvermectinCat. No.:CAS No.:分?式:分?量:作?靶点:作?通路:储存?式:HY-1531070288-86-7C??H??O??875.09Parasite; HIV Integrase; Mitophagy; HSV; AutophagyAnti-infection; Metabolic Enzyme/Protease; AutophagyPowderIn solvent-20°C4°C-80°C-20°C3 years2 years6 months1 monthInhibitors?Agonists?Screening Libraries溶解性数据体外实验DMSO : ≥ 50 mg/mL (57.14 mM)H2O : < 0.1 mg/mL (insoluble)* \Mass1 mg5 mg10 mgSolventConcentration制备储备液1 mM5 mM10 mM1.1427 mL0.2285 mL0.1143 mL5.7137 mL1.1427 mL0.5714 mL11.4274 mL2.2855 mL1.1427 mL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；?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?式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个?内使?，-20°C 储存时，请在 1 个?内使?。体内实验请根据您的实验动物和给药?式选择适当的溶解?案。以下溶解?案都请先按照 In Vitro ?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?作液，建议您现?现配，当天使?； 以下溶剂前显?的百分?是指该溶剂在您配制终溶液中的体积占?；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?式助溶1. 请依序添加每种溶剂：?10% DMSO ?? 40% PEG300 ?? 5% Tween-80 ?? 45% salineSolubility: ≥ 2.5 mg/mL (2.86 mM); Clear solution此?案可获得 ≥ 2.5 mg/mL (2.86 mM，饱和度未知) 的澄清溶液。 以 1 mL ?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? 50 μL Tween-80，混合均匀；然后继续加? 450 μL ?理盐?定容? 1 mL。2. 请依序添加每种溶剂：?10% DMSO ?? 90% corn oilSolubility: ≥ 2.5 mg/mL (2.86 mM); Clear solutionPage 1 of 2 www.MedChemExpress.cn
此?案可获得 ≥ 2.5 mg/mL (2.86 mM，饱和度未知) 的澄清溶液，此?案不适?于实验周期在半个?以上的实验。 以 1 mL ?作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL ??油中，混合均匀。
BIOLOGICAL ACTIVITY
?物活性
Ivermectin (MK-933) 是?种?谱的抗寄??药物，最常?于治疗线?感染，如丝?病，以及疥疮和虱?。Ivermectin (MK-933) 是?种特异性的 Impα/β1 介导的核导?抑制剂，对 HIV-1 和登?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?疱疹病毒 1 (BoHV-1) 复制并抑制 BoHV-1 DNA 聚合酶的核输?。
体外研究
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].
客户使?本产品发表的科研?献
????PLoS Negl Trop Dis.?2019 Aug 20;13(8):e0007681.?????J Anim Physiol Anim Nutr (Berl).?2020 Feb 3.2020See more customer validations on www.MedChemExpress.cnREFERENCES
[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.
McePdfHeightCaution: Product has not been fully validated for medical applications. For research use only.
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