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抑制剂描述:

产品名称:Ivermectin

产品别名:见爱必信官网

英文别名:Ivermectin

靶点:Antiparasitic

CAS:70288-86-7

纯度:97%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Ivermectin is a glutamate-gated chloride channel (GluCls) activator, with antiparasitic activity.

溶解性:DMSO : ≥ 50 mg/mL (57.14 mM)

体外研究:

Ivermectin has potent antiviral activity towards both HIV-1 anddengue 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 binds to a novel site on the GABAA receptor and allosterically enhances the affinity of the GABA binding site in mouse hippocampal embryonic neurons. Ivermectin disrupts neurotransmission processes regulated by GluCl activity by binding to nematode glutamate-gated chloride channels (GluCls). Ivermectin decreases the amount of protein released from microfilariae.

体内研究:Ivermectin (1.25-10 mg/kg, intraperitoneal) significantly reduces 24-h alcohol consumption and intermittent limited access (4-hours) binge drinking, and operant alcohol self-administration (1-h). Ivermectin also produces a significant reduction in 24-h saccharin consumption, but does not alter operant sucrose self-administration. Ivermectin improves mouse survival rate induced by a lethal dose of LPS. Ivermectin significantly decreases the production of TNF-alpha, IL-1ss and IL-6 in vivo and in vitro. Ivermectin suppresses NF-kB translocation induced by LPS.

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