货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
V57001-1ml	10mM in DMSO	￥2240.00 V57001-1ml ￥2240.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

V57001-1ml

10mM in DMSO

￥2240.00

货期：3-5天

产品描述：

Relenopride (YKP10811) hydrochloride is a specific and selective 5-HT4 receptor agonist (Ki=4.96 nM). Relenopride hydrochloride has 120-fold and 6-fold lower affinity, respectively, for 5-HT2A (Ki=600 nM) and 5-HT2B receptors (Ki=31 nM) than for 5-HT4. Relenopride hydrochloride increases gastrointestinal (GI) motility.

靶点：

5-HT2A Receptor;5-HT2B Receptor;5-HT4 Receptor:4.96 nM (Ki);5-HT2A Receptor:600 nM (Ki);5-HT2B Receptor:31 nM (Ki)

体内研究：

Relenopride hydrochloride do not show any significant off-target binding to any other receptors, enzymes, orserotonin-receptor subtypes at 1 μM, except for binding to the 5-HT2A receptor and the 5-HT2B receptor. Relenopride hydrochloride shows antagonist activity at the 5-HT2B receptor with an IC50 of 2.1 μM and no significant activity at the 5-HT2A receptor up to 10 μM. Relenopride hydrochloride shows no activity against serotonin-receptor subtypes 5-HT1B, 5-HT1D, or 5-HT2A at 1 nM to 10 μM, or for serotonin-receptor subtype 5-HT7 at 10 nM to 30 μM.

参考文献：

1. Shin A, et al. A randomized trial of 5-hydroxytryptamine4-receptor agonist, YKP10811, on colonic transit and bowel function in functional constipation. Clin Gastroenterol Hepatol. 2015;13(4):701-8.e1.
2. Yin J, et al. Prokinetic effects of a new 5-HT4 agonist, YKP10811, on gastric motility in dogs. J Gastroenterol Hepatol. 2017;32(3):625-630.
3. Gilet M, et al. Influence of a new 5-HT4 receptor partial agonist, YKP10811, on visceral hypersensitivity in rats triggered by stress and inflammation. Neurogastroenterol Motil. 2014;26(12):1761-1770.

保存条件：

-80°C 6个月; -20°C 1个月,避光,氮气保存

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.889 ml	9.444 ml	18.888 ml
5 mM	0.378 ml	1.889 ml	3.778 ml
10 mM	0.189 ml	0.944 ml	1.889 ml
50 mM	0.038 ml	0.189 ml	0.378 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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