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GSK962040
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。
GSK962040图片
CAS NO:923565-21-3
包装与价格：
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
GSK962040 (GSK962040) 是一种小分子选择性胃动素受体激动剂，pEC50 为 7.9。
Cas No.923565-21-3
别名GSK962040
化学名1-[4-(3-fluoroanilino)piperidin-1-yl]-2-[4-[[(3S)-3-methylpiperazin-1-yl]methyl]phenyl]ethanone
Canonical SMILESCC1CN(CCN1)CC2=CC=C(C=C2)CC(=O)N3CCC(CC3)NC4=CC(=CC=C4)F
分子式C25H33FN4O
分子量424.55
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

GSK962040 is a first small-molecule agonist of motilin receptor with pEC50 value of 7.9 [1].

GSK962040 is discovered as a therapeutic agent for conditions associated with delayed gastric emptying. In the in vitro assay using recombinant human motilin receptor, GSK962040 shows an excellent inhibition activity against motilin receptor with pEC50 value of 7.9. GSK962040 is highly selective against motilin receptor over the human ghrelin receptor and hERG. It also has no significant activity against other receptors including 5-HT, adrenergic, dopamine, histamine and adenosine receptors. In rabbit isolated gastric antrum, GSK962040 is found to enhance the EFS-induced cholinergic contraction and cause a small muscle contraction at high concentration. GSK962040 also induces the contraction of human-isolated stomach preparations at 10μM [1, 2].

References:
[1] Westaway S M, Brown S L, Fell S C M, et al. Discovery of N-(3-Fluorophenyl)-1-[(4-([(3 S)-3-methyl-1-piperazinyl] methyl) phenyl) acetyl]-4-piperidinamine (GSK962040), the First Small Molecule Motilin Receptor Agonist Clinical Candidate. Journal of medicinal chemistry, 2009, 52(4): 1180-1189.
[2] Sanger G J, Westaway S M, Barnes A A, et al. GSK962040: a small molecule, selective motilin receptor agonist, effective as a stimulant of human and rabbit gastrointestinal motility. Neurogastroenterology & Motility, 2009, 21(6): 657-e31.