中文名称: Asimadoline hydrochloride
英文名称: Asimadoline hydrochloride
CAS No: 185951-07-9
分子式: C27H31ClN2O2
分子量: 451
A12777 Asimadoline hydrochloride ≥98% (psaitong)
包装规格:
5mg 10mg 25mg in glass bottle
溶解性:
溶于DMSO(240mg/mL超声)
产品描述:

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:

C27H31ClN2O2

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.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
搜索质检报告(COA)
参考文献 & 客户发表文献

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摩尔浓度计算公式

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稀释公式

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连续稀释计算器方程

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  • 计算结果

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    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):