MK 0677

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Cat.No. 5272 - MK 0677 | C27H36N4O5S.CH3SO3H | CAS No. 159752-10-0
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)
Datasheet
Citations (1)
Literature

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

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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.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

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


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1 Citation 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


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