MK 0677
Chemical Name: 2-Amino-N-[(1R)-2-[1,2-dihydro-1-(methylsulfonyl)spiro[3H-indole-3,4'-piperidin]-1'-yl]-2-oxo-1-[(phenylmethoxy)methyl]ethyl]-2-methylpropanamide methanesulfonate
Purity: ≥98%
Biological Activity
MK 0677 is a high affinity ghrelin receptor agonist (pKi = 8.14). Growth hormone (GH) secretagog; stimulates GH release from rat pituitary cells in vitro (EC50 = 1.3 nM) and enhances GH plasma levels in vivo. Also attenuates isoproterenol-induced lipolysis in rat adipocytes in vitro. Orally bioavailable.Technical Data
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.
Background References
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GH secretagogues and GH releasing peptides act as orthosteric super-agonists but not allosteric regulators for activation of the G protein Galpha(o1) by the Ghrelin receptor.
Bennett et al.
Mol.Pharmacol., 2009;76:802 -
Design and biological activities of L-163,191 (MK-0677): a potent, orally active GH secretagogue.
Patchett et al.
Proc.Natl.Acad.Sci.U.S.A., 1995;92:7001 -
Ghrelin and des-acyl ghrelin both inhibit isoproterenol-induced lipolysis in rat adipocytes via a non-type 1a GH secretagogue receptor.
Mucciolo et al.
Eur.J.Pharmacol., 2004;498:27
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Citations for MK 0677
The citations listed below are publications that use Tocris products. Selected citations for MK 0677 include:
4 Citations: Showing 1 - 4
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Effects of ghrelin receptor activation on forebrain dopamine release, conditioned fear and fear extinction in C57BL/6J mice.
Authors: Ilse Et al.
J Neurochem 2020;154:389-403
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MK0677, a Ghrelin Mimetic, Improves Neurogenesis but Fails to Prevent Hippocampal Lesions in a Mouse Model of Alzheimer's Disease Pathology.
Authors: Jing Et al.
J Alzheimers Dis 2019;72:467-478
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Differential functional selectivity and downstream signaling bias of ghrelin receptor antagonists and inverse agonists.
Authors: John F Et al.
FASEB J 2019;33:518-531
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A novel non-peptidic agonist of the ghrelin receptor with orexigenic activity In vivo
Authors: Pastor-Cavada Et al.
Scientific Reports 2016;6:36456
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