中文名称: Amibegron hydrochloride
英文名称: Amibegron hydrochloride
CAS No: 121524-09-2
分子式: C22H26ClNO4.HCl
分子量: 440.36
A11434 Amibegron hydrochloride ≥98% (psaitong)
包装规格:
5mg in glass bottle
产品描述:

基本信息

产品编号:

A11434

产品名称:

Amibegron hydrochloride

CAS:

121524-09-2

 

储存条件

粉末

-20℃

四年

分子式:

C22H26ClNO4.HCl

溶于液体

-80℃

6个月

分子量:

440.36

-20℃

1个月

化学名: 

Acetic acid,[[(7S)-7-[[(2R)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]-5,6,7,8-tetrahydro-2-naphthalenyl]oxy]-,ethyl ester,hydrochloride (1:1)

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

2.2709mL

11.3543mL

22.7087mL

5mM

0.4542mL

2.2709mL

4.5417mL

10mM

0.2271mL

1.1354mL

2.2709mL

 

生物活性

产品描述

一种选择性的β3-adrenoceptor激动剂,对大鼠结肠β-adrenoceptor的 EC50值为3.5nM;Amibegron hydrochloride具有抗焦虑和抗抑郁的活性。

靶点

EC50:3.5nM (β-adrenoceptor,from rat colon),499nM (β-adrenoceptor,from rat uterus),1.2μM (β2-adrenoceptor,from cerebellum),4.6μM (β1-adrenoceptor1,from cortex)

 

体外研究

Amibegron hydrochloride (SR 58611A) is a selective β-adrenoceptor agonist,with an EC50 of 3.5nM for β-adrenoceptor in rat colon,and 499nM in rat uterus.Amibegron hydrochloride (SR 58611A) shows little effect on β1-and β2-adrenoceptors,5-HT uptake, noradrenaline (NA) uptake,and dopamine (DA) uptake from rat brain tissue,with IC50s of 4.6 and 1.2,0.58,2.5 and 3.2μM,respectively;exhibits no effect on 5-HT1A,5-HT2,MAO-A and MAO-B (IC50>10μM).

体内研究

Amibegron hydrochloride (SR 58611A,0.1 to 0.3mg/kg,i.p.) potentiates the toxicity produced by yohimbine in mice.Amibegron hydrochloride (0.6 and 2mg/kg,i.p.) is also active in the learned helplessness model of antidepressant-like activity in rats.However,Amibegron hydrochloride exhibits no effect on the spontaneous locomotor activity of mice at up to 10mg/kg and of rats at up tp 30mg/kg.Amibegron hydrochloride (3 and 10mg/kg,p.o.) increases the synthesis of 5-HT and tryptophan (Trp) levels in several rodent brain areas such as cortex,hippocampus,hypothalamus,striatum.In addition,Amibegron hydrochloride (10mg/kg,p.o.) promotes the release of 5-HT in rat prefrontal cortex.Systemic (3mg/kg,i.v.) or chronic administration of SR58611A (10mg/kg,p.o.) does not affect the activity of serotonergic neurons in the rat dorsal raphe nucleus.

 

推荐实验方法(仅供参考)

动物实验:

 

Mice

This test is performed on groups of 10-20 mice.Amibegron hydrochloride (0.1 to 0.3mg/kg) or vehicle are administered i.p.30 min before the administration of yohimbine.Yohimbine hydrochloride is administered s.c.at a dose of 30mg/kg always at the same time of day,between 1.30 and 3.30 p.m.Lethality is recorded the next morning at 9 a.m.

Rats

The rats (n=10 per group) are treated randomly according to one of the following protocols:the control sample,which receives no shock,is given vehicle; experimental animals with inescapable shock are treated daily with vehicle or Amibegron hydrochloride (up to 30mg/kg).Animals are treated orally over 5 consecutive days,i.e.6h after shock pretreatment on day 1,and then twice per day,a half dose in the morning (30 min before shuttle-box session) and a half dose in the afternoon (except on the 5th day).Statistical analysis is performed on themean number of escape failures using a two-way analysis of variance followed by Dunnett's test.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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摩尔浓度计算公式

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    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
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