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Relenopride hydrochloride Sale

(Synonyms: YKP10811 hydrochloride) 目录号 : GC63169

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。

Relenopride hydrochloride Chemical Structure

Cas No.:1221416-42-7

规格 价格 库存 购买数量
5 mg
¥2,700.00
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10 mg
¥4,320.00
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25 mg
¥8,550.00
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50 mg
¥13,050.00
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Sample solution is provided at 25 µL, 10mM.

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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.

Chemical Properties

Cas No. 1221416-42-7 SDF
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
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.8888 mL 9.4441 mL 18.8882 mL
5 mM 0.3778 mL 1.8888 mL 3.7776 mL
10 mM 0.1889 mL 0.9444 mL 1.8888 mL
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