中文名称: | Asimadoline hydrochloride | ||||
---|---|---|---|---|---|
英文名称: | Asimadoline hydrochloride | ||||
别名: | 阿西马朵林盐酸盐 EMD-61753 hydrochloride;N-[(1S)-2-[(3S)-3-hydroxy-1-pyrrolidinyl]-1-phenylethyl]-N-methyl-a-phenyl-benzeneacetamide hydrochloride | ||||
CAS No: | 185951-07-9 | 分子式: | C27H31ClN2O2 | 分子量: | 451 |
CAS No: | 185951-07-9 | ||||
分子式: | C27H31ClN2O2 | ||||
分子量: | 451 |
基本信息
产品编号: |
A12777 |
||||
产品名称: |
Asimadoline hydrochloride |
||||
CAS: |
185951-07-9 |
储存条件 |
粉末 |
-20℃ |
四年 |
|
|
||||
分子式: |
溶于液体 |
-80℃ |
6个月 |
||
分子量: |
451.00 |
-20℃ |
1个月 |
||
化学名: |
N-[(1S)-2-[(3S)-3-hydroxy-1-pyrrolidinyl]-1-phenylethyl]-N-methyl-a-phenyl-benzeneacetamide hydrochloride |
||||
Solubility (25°C): |
|||||
体外:
|
DMSO |
|
|||
Ethanol |
|
||||
Water |
|
||||
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 |
2.2173mL |
11.0865mL |
22.1729mL |
5mM |
0.4435mL |
2.2173mL |
4.4346mL |
10mM |
0.2217mL |
1.1086mL |
2.2173mL |
生物活性
产品描述 |
一种口服有效的,选择性的,具有周边活性的κ-opioid激动剂,对豚鼠和人重组κ-opioid的IC50s分别为5.6nM和1.2nM。Asimadoline hydrochloride对血脑屏障的渗透性低,具有外周抗炎作用。Asimadoline hydrochloride可改善糖尿病大鼠的异常性疼痛,并具有用于肠易激综合征(IBS)研究的潜力。 |
|
靶点 |
IC50:5.6nM (guinea pig κ opioid),1.2nM (human recombinant κ opioid) |
|
体外研究 |
Asimadoline (EMD-61753) hydrochloride has high selectively in κ:μ:δ opioid binding ratios of 1:501:498 in human recombinant receptors.The IC50 for Asimadoline hydrochloride binding to μ-opioid receptors is 3µM and to δ-opioid receptors is 0.7µM.The IC50 values for D1,D2,kainate,σ,PCP/NMDA, H1,α1,α2,M1/M2,glycine,5HT1A,5HT1C,5HT1D,5HT2,5HT3,AMPA and kainate/AMPA receptors are all >10µM.Asimadoline hydrochloride has affinity to sodium and L type Ca2+ ion channels at IC50 concentrations 150 to 800 fold the IC50 for the κ receptors.At high concentrations,Asimadoline hydrochloride demonstrates spasmolytic action against 400µM barium chloride in the rat duodenum (IC50=4.2µM),suggesting that Asimadoline hydrochloride may block the direct stimulant effects of barium on smooth muscle through mechanisms that are not identified. |
|
体内研究 |
Asimadoline (EMD-61753 hydrochloride;1,5,15mg/kg;s.c.) acutely ameliorates both formalin-evoked hyperalgesia and tactile allodynia in diabetic rats.The absorption rate following oral administration is 80% in rats and >90% in dogs and monkeys.The metabolism of Asimadoline hydrochloride is rapid and appears similar in animals and man.Asimadoline hydrochloride has peripheral antiinflammatory actions that are partly mediated through increase in joint fluid substance P levels.Treatment with Asimadoline hydrochloride (5mg/kg/day;i.p.) produces marked (and sustained) attenuation of the disease with all three time regimes. |
|
Animal Model: |
Adult female Sprague-Dawley rats |
|
Dosage: |
1,5,15mg/kg |
|
Administration: |
SC;single dose |
|
Result: |
Acutely ameliorated both formalin-evoked hyperalgesia and tactile allodynia in diabetic rats. |
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 )