中文名称: | MK-677(L163191,Ibutamoren) | ||||
---|---|---|---|---|---|
英文名称: | MK-677(L163191,Ibutamoren) | ||||
别名: | 2-amino-2-methyl-N-[(2R)-1-(1-methylsulfonylspiro[2H-indole-3,4'-piperidine]-1'-yl)-1-oxo-3-(phenylmethoxy)propan-2-yl]propanamide mesylate | ||||
CAS No: | 159752-10-0 | 分子式: | C28H40N4O8S2 | 分子量: | 624.77 |
CAS No: | 159752-10-0 | ||||
分子式: | C28H40N4O8S2 | ||||
分子量: | 624.77 |
基本信息
产品编号: |
M10079 |
||||
产品名称: |
MK-677(L163191,Ibutamoren) |
||||
CAS: |
159752-10-0 |
储存条件 |
粉末 |
-20℃ |
四年 |
|
|
||||
分子式: |
溶于液体 |
-80℃ |
6个月 |
||
分子量: |
624.77 |
-20℃ |
1个月 |
||
化学名: |
2-amino-2-methyl-N-[(2R)-1-(1-methylsulfonylspiro[2H-indole-3,4'-piperidine]-1'-yl)-1-oxo-3-(phenylmethoxy)propan-2-yl]propanamide mesylate |
||||
Solubility (25°C): |
|||||
体外:
|
DMSO |
100mg/mL (160.05mM) |
|||
Ethanol |
100mg/mL (160.05mM) |
||||
Water |
100mg/mL (160.05mM) |
||||
体内(现配现用): |
|
||||
<1mg/ml表示微溶或不溶。 |
|||||
普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
|||||
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。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
1.6006mL |
8.0029mL |
16.0059mL |
5mM |
0.3201mL |
1.6006mL |
3.2012mL |
10mM |
0.1601mL |
0.8003mL |
1.6006mL |
50mM |
0.0320mL |
0.1601mL |
0.3201mL |
生物活性
产品描述 |
一种有效的、非肽段类生长激素促分泌素受体(GHSR) 激动剂。 |
靶点 |
GHSR |
体内研究 |
Ibutamoren mesylate (5mg/kg/day) results in a statistically significant increases body weight gain and increases serum IGF1 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 (50μg,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. |
推荐实验方法(仅供参考)
动物实验: |
|
Compounds used are:Ibutamoren mesylate (50μg),octreotide (100μg),and mGH (30μg).Mice are give an initial ip injection (0.1mL) of either saline,octreotide or mGH,followed 10 min later by an ip injection (0.1mL) 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 (0.2mL,1.5M) to serve as positive controls for the immunocytochemistry.Ninety minutes after injection animals are terminally anesthetized with sodium pentobarbitone (60mg/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℃ until processing.Coronal sections of forebrain (40μM) 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 24h at 4℃ 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. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )