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Ivermectin

(Synonyms: 伊维菌素; MK-933) 目录号 : GC12339

伊维菌素 (MK-933) 是一种广谱抗寄生虫剂。

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥399.00
现货
100mg
¥704.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

Ivermectin (MK-933) is a broad-spectrum anti-parasite medication used in humans most commonly to treat nematode infections such as onchocerciasis, as well as scabies and lice. 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).

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].

References:
[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.

Chemical Properties

Cas No. 70288-86-7 SDF
别名 伊维菌素; MK-933
化学名 Ro 5-2807
Canonical SMILES C/C([C@@H](O[C@H]1C[C@H](OC)[C@@H](O[C@H]2C[C@H](OC)[C@@H](O)[C@H](C)O2)[C@H](C)O1)[C@@H](C)/C=C/C=C(CO3)/[C@@]([C@@]3([H])[C@H](O)C(C)=C4)(O)[C@@H]4C5=O)=C\C[C@@H]6C[C@H](O5)C[C@@]7(O[C@@]([C@@H](C)CC)([H])[C@@H](C)CC7)O6
分子式 C48H74O14 分子量 875.09
溶解度 ≥ 43.7545mg/mL in DMSO 储存条件 Store at 2-8°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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