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Submit ReviewMK 0677
Description: High affinity ghrelin receptor agonist
Alternative Names: Ibutamoren mesylate,L-163,191
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% (HPLC)
Biological Activity for MK 0677
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.
Compound Libraries for MK 0677
MK 0677 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for MK 0677
| M. Wt | 624.77 |
| Formula | C27H36N4O5S.CH3SO3H |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 159752-10-0 |
| PubChem ID | 6450830 |
| InChI Key | DUGMCDWNXXFHDE-VZYDHVRKSA-N |
| Smiles | O=S(N2C1=CC=CC=C1C3(CCN(C([C@H](NC(C(C)(N)C)=O)COCC4=CC=CC=C4)=O)CC3)C2)(C)=O.CS(O)(=O)=O |
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.
Solubility Data for MK 0677
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 31.24 | 50 | |
| DMSO | 62.48 | 100 |
Preparing Stock Solutions for MK 0677
The following data is based on the product molecular weight 624.77. 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 | 1.6 mL | 8 mL | 16.01 mL |
| 5 mM | 0.32 mL | 1.6 mL | 3.2 mL |
| 10 mM | 0.16 mL | 0.8 mL | 1.6 mL |
| 50 mM | 0.03 mL | 0.16 mL | 0.32 mL |
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Product Datasheets for MK 0677
References for MK 0677
References are publications that support the biological activity of the product.
Bennett et al (2009) 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. Mol.Pharmacol. 76 802 PMID: 19625579
Patchett et al (1995) Design and biological activities of L-163,191 (MK-0677): a potent, orally active GH secretagogue. Proc.Natl.Acad.Sci.U.S.A. 92 7001 PMID: 7624358
Mucciolo et al (2004) Ghrelin and des-acyl ghrelin both inhibit isoproterenol-induced lipolysis in rat adipocytes via a non-type 1a GH secretagogue receptor. Eur.J.Pharmacol. 498 27 PMID: 15363972
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Keywords: MK 0677, MK 0677 supplier, MK0677, high, affinity, ghrelin, receptors, agonists, growth, hormone, GH, secretagogue, orally, bioavailable, L-163,191, Ibutamoren, mesylate, Ghrelin, Receptors, 5272, Tocris Bioscience
4 Citations for MK 0677
Citations are publications that use Tocris products. Selected citations for MK 0677 include:
Pastor-Cavada et al (2016) A novel non-peptidic agonist of the ghrelin receptor with orexigenic activity In vivo Scientific Reports 6 36456 PMID: 27819353
John F et al (2019) Differential functional selectivity and downstream signaling bias of ghrelin receptor antagonists and inverse agonists. FASEB J 33 518-531 PMID: 30020830
Jing et al (2019) MK0677, a Ghrelin Mimetic, Improves Neurogenesis but Fails to Prevent Hippocampal Lesions in a Mouse Model of Alzheimer's Disease Pathology. J Alzheimers Dis 72 467-478 PMID: 31594237
Ilse et al (2020) Effects of ghrelin receptor activation on forebrain dopamine release, conditioned fear and fear extinction in C57BL/6J mice. J Neurochem 154 389-403 PMID: 32128814
Do you know of a great paper that uses MK 0677 from Tocris? Please let us know.
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Literature in this Area
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.