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Ghrelin 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.
|Storage||Desiccate at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 445.96. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.24 mL||11.21 mL||22.42 mL|
|5 mM||0.45 mL||2.24 mL||4.48 mL|
|10 mM||0.22 mL||1.12 mL||2.24 mL|
|50 mM||0.04 mL||0.22 mL||0.45 mL|
References are publications that support the biological activity of the product.
Esler et al (2007) Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss. Endocrinology 148 5175 PMID: 17656463
Moran and Dailey (2009) Gut peptides: targets for antiobesity drug development? Endocrinology 150 2526 PMID: 19372201
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Keywords: YIL 781, YIL 781 supplier, YIL781, YIL, 781, hydrochloride, ghrelin, receptors, antagonists, GHS-R1a, GHSR, Ghrelin, Receptors, 3959, Tocris Bioscience
3 Citations for YIL 781
Citations are publications that use Tocris products. Selected citations for YIL 781 include:
Tóth et al (2018) Ghrelin receptor antagonism of hyperlocomotion in cocaine-sensitized mice requires βarrestin-2. Synapse 72 PMID: 28941296
Evron et al (2014) G Protein and β-arrestin signaling bias at the ghrelin receptor. J Biol Chem 289 33442 PMID: 25261469
Song et al (2013) Ghrelin modulates lateral amygdala neuronal firing and blocks acquisition for conditioned taste aversion. PLoS One 8 e65422 PMID: 23762368
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