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Submit ReviewMK 0677
说明： High affinity ghrelin receptor agonist
别名： Ibutamoren mesylate,L-163,191
化学名： 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
纯度： ≥98% (HPLC)
生物活性 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.
化合物库 for MK 0677
MK 0677 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for MK 0677
| 分子量 | 624.77 |
| 公式 | C27H36N4O5S.CH3SO3H |
| 储存 | Store at -20°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for MK 0677
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 31.24 | 50 | |
| DMSO | 62.48 | 100 |
制备储备液 for MK 0677
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for MK 0677
参考文献 for MK 0677
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for MK 0677, please let us know.
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关键词: 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 篇 MK 0677 的引用文献
引用文献是使用了 Tocris 产品的出版物。 MK 0677 的部分引用包括：
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
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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.