Chemical Name: 6-(4-Fluorophenoxy)-2-methyl-3-[[(3S)-1-(1-methylethyl)-3-piperidinyl]methyl]-4(3H)-quinazolinone
Biological ActivityGhrelin receptor antagonist (GHS-R1a) (Ki = 17 nM). Displays no significant affinity for the motilin receptor (Ki = 6 μM). Blocks the effects of ghrelin on insulin secretion both in vivo and in vitro. Improves glucose homeostasis in vivo.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss.
Esler et al.
Gut peptides: targets for antiobesity drug development?
Moran and Dailey
Citations for YIL 781
The citations listed below are publications that use Tocris products. Selected citations for YIL 781 include:
2 Citations: Showing 1 - 2
G Protein and β-arrestin signaling bias at the ghrelin receptor.
Authors: Evron Et al.
J Biol Chem 2014;289:33442
Ghrelin modulates lateral amygdala neuronal firing and blocks acquisition for conditioned taste aversion.
Authors: Song Et al.
PLoS One 2013;8:e65422
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