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抑制剂描述： 产品名称：Monepantel 产品别名：见爱必信官网 英文别名：Monepantel 靶点：AChR CAS：887148-69-8 纯度： 外观：见爱必信官网 保存方法： 描述：Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits. 溶解性：10 mM in DMSO 体外研究： The metallocenyl analogues of monepantel shows nematocidal activity. Monepantel (25 μM) induces accumulation of acidic vacuoles. Ovarian cancer cell lines are highly sensitive to Monepantel with IC50 values of 7.2±0.2 μM (OVCAR-3) and 10.5±0.4 μM (A2780). Monepantel (0, 10 and 25 μM) induces autophagosome formation in these cancer cell lines. Monepantel (0, 10 and 25 μM) exhibits a markedly reduced level of punctate staining indicating the suppression of phosphorylated mTOR at Ser2448. Monepantel also decreases the expression of phosphorylated Raptor at Ser792, which is one of the mTORC1 coMonepantelex members. Monepantel (250 μg/mL) leads multiple ABC transporter genes higher transcription in both worm isolates. Larvae exposed to monepantel at 250 μg/mL shows an increased efflux of rhodamine-123 and a proportion of the larval population shows an ability to subsequently tolerate higher concentrations of IVM in migration assays. 体内研究：Monepantel (10 μM) significantly increased all CYP-related activities and CYP3A24 mRNA in sheep.
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