中文名称: 安倍生坦
英文名称: Ambrisentan
CAS No: 177036-94-1
分子式: C22H22N2O4
分子量: 378.43
A10985 安倍生坦 ≥98% (psaitong)
包装规格:
250mg 1g in glass bottle
溶解性:
溶于DMSO
产品描述:

基本信息

产品编号:

A10985 

产品名称:

Ambrisentan

CAS:

177036-94-1

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C22H22N2O4

溶于液体

-80℃

6个月

分子量:

378.43

-20℃

1个月

化学名: 

(S)-2-((4,6-dimethylpyrimidin-2-yl)oxy)-3-methoxy-3,3-diphenylpropanoic acid

Solubility (25°C):

 

体外:

 

DMSO

75mg/mL (198.19mM)

Ethanol

6mg/mL (15.85mM)

Water

Insoluble

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

2.6426mL

13.2128mL

26.4257mL

5mM

0.5285mL

2.6426mL

5.2851mL

10mM

0.2643mL

1.3213mL

2.6426mL

50mM

0.0529mL

0.2643mL

0.5285mL

 

生物活性

产品描述

一种选择性的ET A型受体拮抗剂。

靶点

ETA receptor

 

体外研究

Ambrisentan is an endothelin type A receptor antagonist.Ambrisentan induces Nrf2 activation.Endothelial permeability increased in BMEC monolayers at 24h of hypoxia exposure and compared to vehicle control,Ambrisentan attenuates hypoxia-induced BMEC leak.These results are reversed when prior to treatment BMEC are transfected with siRNA against Nrf2.

体内研究

In the Ambrisentan group,hepatic hydroxyproline content is significantly lower than in the control group (18.0μg/g±6.1μg/g vs 33.9μg/g±13.5μg/g liver,respectively,P=0.014).Hepatic fibrosis estimated by Sirius red staining and areas positive for αsmooth muscle actin,indicative of activated hepatic stellate cells,are also significantly lower in the Ambrisentan group (0.46%±0.18% vs 1.11%±0.28%,respectively,P=0.0003;and 0.12%±0.08% vs 0.25%0.11%,respectively,P=0.047).Moreover,hepatic RNA expression levels of procollagen-1 and tissue inhibitor of metalloproteinase-1 (TIMP-1) are significantly lower by 60% and 45%,respectively,in the Ambrisentan group.Inflammation,steatosis,and endothelin-related mRNA expression in the liver are not significantly different between the groups.Ambrisentan attenuates the progression of hepatic fibrosis by inhibiting hepatic stellate cell activation and reducing procollagen-1 and TIMP-1 gene expression.Ambrisentan did not affect inflammation or steatosis.

 

推荐实验方法(仅供参考)

细胞实验:

 

Unless otherwise stated,for each BMEC experiment cells are randomly divided into 4 groups:(1) normoxia vehicle control (Nx-CTRL);(2) normoxia-treated;(3) hypoxia (24h) control (Hx-CTRL) and (4) hypoxia (24h) treated.As previously described,Nrf2 activators are added 24h prior to any hypoxic exposures.Cell treatments are;Protandim (100μg/mL),methazolamide (125μg/mL,nifedipine (7μg/mL) or Ambrisentan (40μg/mL).In addition,some cells are treated with Nrf2 siRNA.In these experiments,siRNA is added 24h prior to drug treatments.The rationale for 24 h hypoxia exposure for BMEC is to ensure that cells remained transfected with siRNA for the pre-treatment of drugs (24h in normoxia) and during the 24h hypoxia exposure.Data is collected from at least three separate cell culture preparations on three separate days (n=9).

 

动物实验:

 

Mice

A total of 13 male FLS-ob/ob mice (age,8 wk;body weight,42.88 g±1.74g) are used.At the age of 12 wk,male FLS-ob/ob mice are randomly assigned to the Ambrisentan (n=8) or control (n=5) group.Intragastric gavage administration is carried out in conscious animals with an appropriately sized gastric tube.Ambrisentan (2.5mg/kg per day) is orally administered every afternoon for 4 wk as a bolus through a gastric tube.Water is administered to the control group.At week 4,animals are fasted for 4h and tail vein blood is drawn and subjected to blood glucose determination.Animals are killed by pentobarbital anesthesia injection after 4 wk and blood is collected from the right ventricle.Plasma samples are frozen and stored at -80℃ Liver and visceral fat are then weighed,snap-frozen in liquid nitrogen,and stored at -80℃.Additional liver specimens are fixed in 10% buffered formalin and embedded in paraffin for histological analysis.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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