Ibutamoren mesylate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种非肽类、强效、选择性、口服活性的生长素释放肽受体 (GHSR) 激动剂，EC50 为 1.3 nM（从大鼠垂体细胞中释放 GH）。

A non-peptidic, poten and selective, orally-active agonist of the ghrelin receptor (GHSR) with EC50 of 1.3 nM (releases GH from rat pituitary cells); significantly increased peak GH concentrations 20.4-fold at 0.25 mg/kg in beagles; has shown to sustain activation of GH-IGF-1 Axis and increase in lean body mass but no change in total fat mass or visceral fat.Growth Hormone Deficiency Phase 2 Clinical(In Vivo):Ibutamoren mesylate (5 mg/kg/day) results in a statistically significant increases body weight gain and increases serum IGF-1 and GH levels in dogs. Ibutamoren mesylate results in no significant increase in CSF IGF-1 or GH levels on days 7 or 15 of the study. Pretreating mice with GH blocks activation of these neurons by Ibutamoren mesylate (50 μg, i.p.). In the knockout mice, both GH and octreotide fail to inhibit Ibutamoren mesylate activation of arcuate neurons. Chronic oral administration of MK-0677 is associated with significant increases in GH and IGF-I levels that are maintained for the duration of the treatment. The GH profile following MK-0677 administration consists of episodic increases above control. MK-0677 significantly increases peak GH concentrations after oral administration. MK-0677 is a potent GH secretagogue that induces an immediate, large, long lasting increase in GH levels when administered orally or i.v.

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MK-677 | MK-0677 | L-163191

GPCR/G Protein

GHSR

GHSR

Endocrinology

Growth Hormone Deficiency

159752-10-0

624.7692

C28H40N4O8S2

>98% (HPLC)

10 mM in DMSO

CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CN(C4=CC=CC=C34)S(=O)(=O)C)N.CS(=O)(=O)O

Propanamide, 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-methyl-, methanesulfonate (1:1)

(-20℃)

With Ice Pack

≥ 2 years