Ivermectin-MK-933-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIvermectinCat. No.: HY-15310CAS No.: 70288-86-7Synonyms: MK-933分式: CHO分量: 875.09作靶点: Parasite; HIV Integrase; Mitophagy; Autophagy作通路: Anti-infection; Metabolic Enzyme/Protease; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solv

2、ent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (57.14 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (2.86 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (2.86 mM); Clear solutionBIOLOGICAL ACTIVIT

3、Y物活性 Ivermectin (MK-933)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) 种特异性的 Imp/1 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 7 nAChRs 的正异构效应物。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

4、 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 agonista,b-methylene-ATP in a use- and voltage-independent manner without changing the ion selectivity of P2X4channels 1.Ivermectin (MK-933

5、) 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 Imp/1 to NS5 (IC50=17 M), but not of Imp1 alone toNS5 3.Ivermectin (MK-933) has potent antiviral a

6、ctivity towards both HIV-1 and dengue virus, both of which arestrongly reliant on importin / nuclear import, with respect to the HIV-1 integrase and NS5 (non-structuralprotein 5) polymerase proteins respectively 3.REFERENCES1. Khakh BS, et al. Allosteric control of gating and kinetics at P2X(4) rece

7、ptor 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 /-mediated nuclear import able to inhibit replication of HIV-1 anddengue virus. Biochem J. 2012 May 1;443(3):851-6.McePdfHeightCaution: Product has not been fully validated for medical applications.For researc