货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
S85468-5mg	≥99%	￥800.00 S85468-5mg ￥800.00 3-5天	0 货期：3-5天	-	-	-	-
S85468-10mg	≥99%	￥1170.00 S85468-10mg ￥1170.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

Lu AE58054 hydrochloride is an in-vivo binding affinity and effect, in-vitro selectivity and potency of 5-HT(6)R antagonist (Ki: 0.83 nM).

靶点：

5-HT Receptor;5-HTReceptor

体外研究：

In the 5-HT(6) GTP gamma S efficacy assay, Lu AE58054 showed potent inhibition of 5-HT-mediated activation. Apart from medium affinity to adrenergic alpha (1B)- and alpha(1A)-adrenoreceptors, Lu AE58054 shows >50-fold selectivity compared with more than 70 targets examined

体内研究：

In the rats model, Orally administered Lu AE58054 inhibited binding of the 5-HT6 antagonist Lu AE60157 (ED50: 2.7 mg/kg). Administration of Lu AE58054 in a dose range (5–20 mg/kg) leading to above 65% 5-HT6R binding, which reversed cognitive impairment in rats treatment with phencyclidine. These results indicate that Lu AE58054 is a potent antagonist of 5-HT6Rs with good oral bioavailability in the rat model of cognitive impairment in schizophrenia

参考文献：

1. Louise Witten, Benny Bang-Andersen, et al. Characterization of [3H]Lu AE60157 ([3H]8-(4-methylpiperazin-1-yl)-3-phenylsulfonylquinoline) binding to 5-hydroxytryptamine6 (5-HT6) receptors in vivo, European Journal of Pharmacology, Volume 676, Issues 1–3, 2012, Pages 6-11. 2. Arnt J, Bang-Andersen B, Grayson B, et al. Lu AE58054, a 5-HT6 antagonist, reverses cognitive impairment induced by subchronic phencyclidine in a novel object recognition test in rats. Int J Neuropsychopharmacol, 2010, 13(8): 1021-1033.

溶解性：

Soluble in DMSO、H2O、Ethanol

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.3 ml	11.499 ml	22.997 ml
5 mM	0.46 ml	2.3 ml	4.599 ml
10 mM	0.23 ml	1.15 ml	2.3 ml
50 mM	0.046 ml	0.23 ml	0.46 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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Lu AE58054 (Hydrochloride)