中文名称: Aminaftone
英文名称: Aminaftone
CAS No: 14748-94-8
分子式: C18H15NO4
分子量: 309.32
A11469 Aminaftone (psaitong)
包装规格:
100mg in glass bottle
产品描述:

基本信息

产品编号:

A11469

产品名称:

Aminaftone

CAS:

14748-94-8

 

储存条件

粉末

-20℃

四年

分子式:

C18H15NO4

溶于液体

-80℃

二年

分子量:

309.32

 

 

化学名: 

(1,4-dihydroxy-3-methylnaphthalen-2-yl) 4-aminobenzoate

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。

 

生物活性

产品描述

一种4-氨基苯甲酸的衍生物,通过干扰pre-pro-ET-1基因转录,而下调内皮素-1(ET-1)产生。

靶点

endothelin-1(ET-1)

 

体外研究

Aminaftone inhibits Endothelin-1 (ET-1) production in cell cultures by interfering with transcription of the pre-proendothelin-1 (PPET-1) gene.Incubation with IL-1beta increases concentrations of ET-1 and PPET-1 relative gene expression.Incubation with Aminaftone significantly reduces production of ET-1 in a concentration-dependent manner.A strong direct correlation is found between ET-1 concentrations and PPET-1 relative gene expression,but Aminaftone does not influence endothelin-converting enzyme (ECE) activity.

体内研究

The rats are randomly assigned to the following experimental groups:Control;Monocrotaline;Aminaftone 30mg/kg/day;Aminaftone 150mg/kg/day.After 5 weeks,mortality is significantly lower in the animals treated with Aminaftone at both doses compared to Monocrotaline alone.Aminaftone reduces plasma concentration of ET-1 and seems to reduce right heart hypertrophy and the wall thickness of the pulmonary arteries at the highest dose.At the end of the experiment,no rats die in the control and Aminaftone 150 groups,while mortality is 38% in the Monocrotaline group and 13% in the Aminaftone 30 group.Overall,Aminaftone treated rats have a significantly lower mortality compared to rats in the Monocrotaline group (P=0.044).

 

推荐实验方法(仅供参考)

细胞实验:

 

Human ECV304 endothelial cells are incubated with interleukin-1beta (IL-1beta) 100 IU/mL with or without the addition of increasing concentrations of Aminaftone (2,4 or 6μg/mL).ET-1 concentrations in surnatants are quantified by enzyme immunoassay kit at 3,6 and 12 hours.PPET-1 gene expressions are also analysed by real-time polymerase chain reaction (RT-PCR) at the same time points.ECE activity is also determined.

 

动物实验:

 

Rats

Male Wistar rats weighing 300±30g are randomly assigned to one of the following four experimental groups:1) control healthy rats (n=11);2) only injection of Monocrotaline (n=12);3) injection of Monocrotaline followed by Aminaftone 30mg/kg treatment (Aminaftone30) (n=8);and 4) injection of Monocrotaline followed by Aminaftone 150mg/kg treatment (Aminaftone150) (n=8).Aminaftone is administered as food admix.Rats are weighed twice a week.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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    C8=C7/X C8: LOG(C8):