Ibutamoren Mesylate

Ibutamoren Mesylate (MK-0677) 是非肽段类生长激素促分泌素受体 (GHSR) 激动剂,也是一种口服有活性的生长激素 (GH) 促分泌素。

CAS号

159752-10-0

分子式

C28H40N4O8S2

主要靶点

GHSR

仅限科研使用

Cat No : CM04228

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Synonyms

伊布莫仑甲磺酸盐|MK-677|MK-0677



产品信息

Ibutamoren Mesylate is a potent, non-peptide Growth hormone secretagogue receptor (GHSR) agonist.

CAS号 159752-10-0
分子式 C28H40N4O8S2
主要靶点 GHSR
主要通路 G蛋白偶联受体
分子量 624.77
纯度 98.00%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 伊布莫仑甲磺酸盐|MK-677|MK-0677

体内活性

Following oral administration Ibutamoren Mesylate(MK0677) amplifies episodic GH release.?Mechanistically, it synergizes with growth hormone releasing hormone (GHRH) through a receptor and signal transduction pathway distinct from that of GHRH and is a functional antagonist of somatostatin (SRIF).?MK0677 also acts on the arcuate nucleus and appears to stimulate GHRH release.?By using 35S-MK0677, a new G-protein coupled receptor for MK0677 was characterized in the plasma membrane fraction of pituitary and hypothalamic tissue.?The receptor is present in very low abundance and couples to phospholipase C. Other ligands selective for this receptor also cause synchronization of well-defined pathways leading to GH release.?Repeated oral treatment of dogs once daily with MK0677 initiates amplified pulsatile GH release accompanied by increases in IGF-1 that are sustained.?The unique biological properties of MK0677 and other synthetic ligands that bind to the same receptor force us to predict that these ligands mimic a naturally occurring hormone that regulates pulsatile GH release[1].

溶解度

DMSO:50 mg/mL (80.03 mM)

参考文献

1.Smith R G , Pong S S , Hickey G , et al. Modulation of pulsatile GH release through a novel receptor in hypothalamus and pituitary gland[J]. Recent Progress in Hormone Research, 1996, 51:261-85; discussion 285-6.
2.Aydemir M , Durap F , Kayan C , et al. Insulin-Like Growth Factor-1 and Growth Hormone (GH) Levels in Canine Cerebrospinal Fluid are Unaffected by GH or GH Secretagogue (MK-0677) Administration[J]. Hormone and Metabolic Research, 1999, 31(02/03):133-137.

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