Relenopride hydrochloride

立即咨询

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。

CAS NO:

1221416-42-7

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议

产品介绍

Relenopride (YKP10811) hydrochloride 是一种特异性和选择性的 5-HT4 受体激动剂 (Ki=4.96 nM)。与5-HT4相比，Relenopride hydrochloride 对 5-HT2A (Ki=600 nM)和5-HT2B (Ki=31 nM) 受体的亲和力分别低 120 倍和 6 倍。Relenopride hydrochloride 增加胃肠运动。

Cas No.	1221416-42-7
别名	YKP10811 hydrochloride
分子式	C₂₄H₃₁Cl₂FN₄O₄
分子量	529.43
溶解度	DMSO : 110 mg/mL (207.77 mM; Need ultrasonic)
储存条件	Store at -20°C, protect from light, stored under nitrogen
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
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[1][2]. 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[1]. [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.