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Ivermectin B1a
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ivermectin B1a图片
CAS NO:71827-03-7
包装与价格:
包装价格(元)
5mg电议
25mg电议

产品介绍
伊维菌素 B1a 是阿维菌素 B1a 的衍生物,是伊维菌素的主要成分。
Cas No.71827-03-7
别名伊维菌素 B1a
化学名5-O-demethyl-22,23-dihydro-avermectin A1a
Canonical SMILESC/C([C@@H](O[C@@]1([H])C[C@H](OC)[C@@H](O[C@]2([H])O[C@@H](C)[C@H](O)[C@@H](OC)C2)[C@H](C)O1)[C@@H](C)/C=C/C=C(CO3)/[C@@]([C@@]3([H])[C@H](O)C(C)=C4)(O)[C@]4([H])C5=O)=C\C[C@]6([H])C[C@@](O5)([H])C[C@]7(CC[C@H](C)[C@]([C@H](CC)C)([H])O7)O6
分子式C48H74O14
分子量875.1
溶解度Soluble in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Ivermectin B1a is the main component (not less than 80%) of the anthelmintic, ivermectin. Ivermectin is one of the most useful veterinary antiparasitic drugs ever produced. Ivermectin belongs to the macrocyclic lactone class of avermectins. Ivermectin contains two homologous compounds, H2B1a and H2B1b. Avermectins are potent insecticidal, anthelmintic and acaricidal compounds in mediating the paralysis of nematodes and certain classes of ectoparasites by increasing the membrane permeability to chlorine ions[1].

In humans, ivermectin has been used to treat African river blindness (onchocerciasis). Ivermectin significantly decreased the prevalence of skin and eye diseases linked to this infection [2]. Ivermectin B1a produced antiparasitic activity via an interaction with a common receptor molecule, glutamate-gated chloride channels, which virtually expressed on nematode neurons and pharyngeal muscle cells, inducing irreversible channel opening and very long-lasting hyperpolarization/depolarization of the neuron/muscle cell, thereby blocking further function. The EC50 of ivermectin was 104 nM [1,3].

References:
[1] J.  Wolsetnholme and A. T. Rogers. Glutamate-gated chloride channels and the mode of action of the avermectin/milbemycin anthelmintics. Parasitology131 Suppl, S85-S95 (2005).
[2] S.  Gaisser, L. Kellenberger, A. L. Kaja, et al. Direct production of ivermectin-like drugs after domain exchange in the avermectin polyketide synthase of Streptomyces avermitilis ATCC31272. Organic & Biomolecular Chemistry 1(16), 2840-2847 (2003).
[3] J.  P. Arena, K. K. Liu, P. S. Paress, et al. The mechanism of action of avermectins in Caenorhabditis elegans: Correlation between activation of glutamate-sensitive chloride current, membrane binding, and biological activity. Journal of Parasitology 81, 286-294 (1995).