Ivermectin

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Chemical Structure| 70288-86-7 同义名 : 伊维茵素 ;MK-933; 22,23-dihydro Avermectin B1; Pandex; Noromectin; MK-0933; 1 Mectizan; L 64047; Ivomec; CD-5024; K-237
CAS号 : 70288-86-7
货号 : A292838
分子式 : C48H74O14
纯度 : 98%
分子量 : 875.09
MDL号 : MFCD00869511
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Ivermectin (IVM), a widely used antiparasitic agent in human and veterinary medicine. Ivermectin (MK-933) activates glutamate-gated chloride channels in the nerves and muscles of the parasite, leading to membrane hyperpolarization and muscle paralysis[3]. Ivermectin is a specific positive allosteric effector of heterologously expressed P2X(4) and possibly of heteromeric P2X(4)/P2X(6) channels. In the submicromolar range (EC50 = 250 nM) the action of Ivermectin is rapid and reversible, resulting in increased amplitude and slowed deactivation of P2X4 channel currents evoked by ATP. Ivermectin also markedly increased the potency of ATP and that of the normally low-potency agonist alpha, beta-methylene-ATP in a use- and voltage-independent manner without changing the ion selectivity of P2X(4) channels[4]. Ivermectin 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. Ivermectin strongly inhibits the binding of Impα/β1 to NS5 (IC50 = 17 μM), but not of Impβ1 alone to NS5[5]. Ivermectin also inhibits bovine herpesvirus 1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00342576 - Completed - India ... 展开 >> Tuberculosis Research Centre Chennai, India 收起 <<
NCT02644525 Loaisis Phase 2 Not yet recruiting June 30, 2019 Cameroon ... 展开 >> Centre de Recherche sur les Filarioses et Autres Maladies Tropicales Not yet recruiting Mbalmayo, Cameroon Contact: Joseph Kamgno, M.D.    Not Listed    kamgno@crfilmt.org 收起 <<
NCT01080989 Flavivirus Infection ... 展开 >> Alphavirus Infections Malaria Parasitic Disease Leptospirosis Hypertension Metabolic Syndromes 收起 << Not Applicable Completed - Taiwan ... 展开 >> Kaoshing Medical University Chung-Ho Memorial Hospital Kaoshiung, Taiwan 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.14mL

0.23mL

0.11mL

5.71mL

1.14mL

0.57mL

11.43mL

2.29mL

1.14mL
参考文献

[1]Wagstaff KM, Sivakumaran H, 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.

[2]Reiter RJ. Oxidative damage in the central nervous system: protection by melatonin. Prog Neurobiol. 1998 Oct;56(3):359-84.

[3]Priel A, Silberberg SD. Mechanism of ivermectin facilitation of human P2X4 receptor channels. J Gen Physiol. 2004;123(3):281-293

[4]Khakh BS, Proctor WR, Dunwiddie TV, Labarca C, Lester HA. Allosteric control of gating and kinetics at P2X(4) receptor channels. J Neurosci. 1999;19(17):7289-7299

[5]Wagstaff KM, Sivakumaran H, Heaton SM, Harrich D, Jans DA. 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;443(3):851-856

[6]Raza S, Shahin F, Zhai W, et al. Ivermectin Inhibits Bovine Herpesvirus 1 DNA Polymerase Nuclear Import and Interferes with Viral Replication. Microorganisms. 2020;8(3):409. Published 2020 Mar 13