Ibutamoren Mesylate

目录号: GC10287纯度: >98.00%同义词: 伊布莫仑甲磺酸盐; MK-677; MK-0677

A growth hormone secretagogue and ghrelin receptor agonist


Ibutamoren Mesylate
Cas No.: 159752-10-0
规格价格库存数量操作
10mg¥675.00现货
1
50mg¥1,188.00现货
1

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产品描述 Description

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

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[1]. 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[2]. 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[3]. 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[4]

Reference:
[1]. Prahalada S, 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. Horm Metab Res. 1999 Feb-Mar;31(2-3):133-7.
[2]. Zheng H, et al. Somatostatin receptor subtype 2 knockout mice are refractory to growth hormone-negative feedback on arcuate neurons. Mol Endocrinol. 1997 Oct;11(11):1709-17.
[3]. Hickey GJ, et al. Repeat administration of the GH secretagogue MK-0677 increases and maintains elevated IGF-I levels in beagles. J Endocrinol. 1997 Feb;152(2):183-92.
[4]. Jacks T, et al. MK-0677, a potent, novel, orally active growth hormone (GH) secretagogue: GH, insulin-like growth factor I, and other hormonal responses in beagles. Endocrinology. 1996 Dec;137(12):5284-9.

实验参考方法 Experimental Reference Method

Animal experiment:

Compounds used are: Ibutamoren mesylate (50 μg), octreotide (100 μg), and mGH (30 μg). Mice are give an initial ip injection (0.1 mL) of either saline, octreotide or mGH, followed 10 min later by an ip injection (0.1 mL) of either saline or Ibutamoren mesylate. Thus, the first study comprised of the following groups: saline/saline, saline/Ibutamoren mesylate, mGH/saline, mGH/Ibutamoren mesylate saline/saline, saline/Ibutamoren mesylate, mGH/saline, mGH/Ibutamoren mesylate, and the second study of: saline/saline, saline/Ibutamoren mesylate, octreotide/saline, octreotide/Ibutamoren mesylate. Additionally, a number of mice are injected ip with hypertonic saline (0.2 mL, 1.5 M) to serve as positive controls for the immunocytochemistry. Ninety minutes after injection animals are terminally anesthetized with sodium pentobarbitone (60 mg/kg, ip) and perfused transcardially with heparinized saline followed by 4% paraformaldehyde in 0.1mol/Lphosphate buffer (PB, pH 7.4). Brains are then removed and placed in the same solution for 24 h before being stored at− 80°C until processing. Coronal sections of forebrain (40 μM) are cut on a freezing microtome and placed in 0.1mol/LPB containing Triton X-100 (PB-T, pH 7.4). Sections are incubated for 24 h at 4°C in Ab-2 Fos antibody (rabbit polyclonal; 1:1000 in 1% normal sheep serum). The antibody-antigen complex is localized with a 1-h incubation in biotinylated anti-rabbit Ig, followed by a 1-h incubation in avidin, biotinylated horseradish peroxidase. The reaction product is visualized using a glucose oxidase-diaminobenzidine-nickel method, and Fos-like immunoreactivity is visualized as a dense purple-black precipitate restricted to the nucleus. The number of c-fos positive nuclei in the arcuate and periventricular nuclei (six to eight sections per mouse) are counted double-blind and a group mean calculated (mean±sem). Statistical analysis is performed by a two-way ANOVA followed by an all pairwise multiple comparison of data with significance taken as P < 0.05.

References:

[1]. Prahalada S, 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. Horm Metab Res. 1999 Feb-Mar;31(2-3):133-7.
[2]. Zheng H, et al. Somatostatin receptor subtype 2 knockout mice are refractory to growth hormone-negative feedback on arcuate neurons. Mol Endocrinol. 1997 Oct;11(11):1709-17.
[3]. Hickey GJ, et al. Repeat administration of the GH secretagogue MK-0677 increases and maintains elevated IGF-I levels in beagles. J Endocrinol. 1997 Feb;152(2):183-92.
[4]. Jacks T, et al. MK-0677, a potent, novel, orally active growth hormone (GH) secretagogue: GH, insulin-like growth factor I, and other hormonal responses in beagles. Endocrinology. 1996 Dec;137(12):5284-9.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
159752-10-0
同义词
伊布莫仑甲磺酸盐; MK-677; MK-0677
化学名
2-amino-2-methyl-N-[(2R)-1-(1-methylsulfonylspiro[2H-indole-3,4'-piperidine]-1'-yl)-1-oxo-3-phenylmethoxypropan-2-yl]propanamide;methanesulfonic acid
SMILES
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
分子式
C28H40N4O8S2
分子量
624.77 g/mol
溶解性
DMF: 25 mg/ml,DMSO: 25 mg/ml,Ethanol: 10 mg/ml,PBS (pH 7.2): 10 mg/ml
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol