Biological Activity
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
MK 0677 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 624.77 |
| Formula | C27H36N4O5S.CH3SO3H |
| Storage | Store at +4°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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 62.48 | 100 | |
| water | 31.24 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 624.77. Batch specific molecular weights may vary from batch to batch due to solvent 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
References
References are publications that support the products' biological activity.
Bennett et al (2009) Growth hormone secretagogues and growth hormone 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 growth hormone 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 growth hormone secretagogue receptor. Eur.J.Pharmacol. 498 27 PMID: 15363972
Keywords: MK 0677, supplier, MK0677, high, affinity, ghrelin, receptors, agonists, growth, hormone, GH, secretagogue, orally, bioavailable, L-163,191, Ibutamoren, mesylate, L-163,191, Ghrelin, Receptors, Ghrelin, Receptors, Tocris Bioscience
