Catalog Number: 3959
Chemical Name: 6-(4-Fluorophenoxy)-2-methyl-3-[[(3S)-1-(1-methylethyl)-3-piperidinyl]methyl]-4(3H)-quinazolinone
Biological Activity
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.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in water
  • Purity:
  • Storage:
    Desiccate at RT
  • CAS No:
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.
Background References
  1. Gut peptides: targets for antiobesity drug development?
    Moran and Dailey
    Endocrinology, 2009;150:2526
  2. Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss.
    Esler et al.
    Endocrinology, 2007;148:5175
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