中文名称: CGS 21680
英文名称: CGS 21680
CAS No: 120225-54-9
分子式: C23H29N7O6
分子量: 499.52
C10969 CGS 21680 ≥98% (psaitong)
包装规格:
10mg in glass bottle
产品描述:

基本信息

产品编号:

C10969

产品名称:

CGS 21680

CAS:

120225-54-9

 

储存条件

粉末

2-8℃

四年

分子式:

C23H29N7O6

溶于液体

-80℃

二年

分子量:

499.52

 

 

化学名: 

2-[4-(2-Carboxyethyl)phenylethylamino]-5'-(N-ethyl)carboxamidoadenosine

Solubility (25°C):

 

体外:

 

DMSO

100mg/mL (186.57mM)

Ethanol

Insoluble

Water

Insoluble

体内(现配现用):

5% DMSO+40% PEG 300+5% Tween 80+50%dd H2O

5mg/mL

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

1.8657mL

9.3287mL

18.6574mL

5mM

0.3731mL

1.8657mL

3.7315mL

10mM

0.1866mL

0.9329mL

1.8657mL

50mM

0.0373mL

0.1866mL

0.3731mL

 

生物活性

产品描述

一种选择性的adenosine A2A receptor特异性激动剂,Ki值为27nM。

靶点

Adenosine A2 receptor
(in rat brain tissue)

22nM

 

体外研究

CGS21680 significantly upregulates CD39 and CD73 expression.CGS21680 accelerates the adenosine triphosphate (ATP) hydrolysis and adenosine generation.CGS21680 (10nM) alone shows only small survival activity,but the activity is significantly enhanced by the addition of a phosphodiesterase inhibitor,IBMX.The survival activity of CGS21680 on cultured motoneurons is exerted by mixed effects of the adenylate cyclase-cAMP-PKA pathway and the transactivation of neurotrophin receptors.

体内研究

CGS21680 (1mg/kg/i.p.) intervention promotes the development of EAN.CGS21680 exacerbates experimental autoimmune neuritis in Lewis rats induced with bovine peripheral myelin.The exacerbation is accompanied with reduced CD4+Foxp3+Tcells,increased CD4+CXCR5+Tcells,Bcells,dendritic cells and antigen-specific autoantibodies,which is possibly due to the inhibition of IL-2 induced by CGS21680.CGS21680 (0.1mg/kg,i.p.) transiently increases heart frequency but does not modify blood pressure of rat,and does not modify either heart frequency or blood pressure at 0.01mg/kg.Following transient MCAo,CGS21680 at both doses protects from neurological deficit from the first day up to 7 days thereafter.At this time,it has reduced microgliosis,astrogliosis and improved myelin organization in the striatum and cytoarchitecture of the ischemic cortex and striatum.Two days after transient MCAo,CGS21680 has reduced the number of infiltrated granulocytes into the ischemic tissue.

 

推荐实验方法(仅供参考)

激酶实验:

放射性配体结合试验

A2受体结合的测定通过在ADA预处理的大鼠纹状体膜中测定,用[3H]NECA (比活度,20 Ci/mmol),在50nM 环戊基腺苷存在下阻断A受体,100μM 2-CADO存在下识别非特异性结合。反应条件与评估[3H]CHA结合的条件是一致的,除了缓冲液中也含有10mM MgC12。终反应体积是2ml,含有的[3H]NECA终浓度是2nM。

 

细胞实验:

 

10×106 MNCs from each group are re-suspended in 2mL RPMI 1640.Cell suspensions are added with carboxy-fluorescein diacetate,succinimidyl ester (CFSE,final concentration 2.5μM) and thoroughly mixed.After incubation in the dark for 15 min at 37℃,the staining process is quenched by adding 10mL ice-cold complete RPMI 1640 (containing 10% FBS) and incubated on ice for 5 min.Then cells are washed twice with RPMI 1640.Cell pellets are re-suspended in complete RPMI 1640 (containing 10% FBS).The stained MNCs (1×106 cells/mL,1mL/well) are cultured in triplicates in 24-well culture plates in the dark at 37℃.Each well is supplied with 50μL of Concanavalin A (ConA,final concentration 5μg/mL) or 50μL of P0 peptide (final concentration 10μg/mL).72h later,cells are collected and stained with PE-labeled anti-rat CD4 antibody for 30 min at 4℃.Finally,cells are analyzed with a flow cytometer

 

动物实验:

 

Female Lewis rats aged 6-8 weeks (body weight,140-160g) are housed under specific pathogen-free conditions in the local animal facility with free access to water and food.Administration of CGS21680 (at a dose of 1mg/kg in PBS) starts on day 5p.i.Rats in experimental group are injected with CGS21680 intraperitoneally (i.p.) every two days until the end of the experiments.Rats in control group are given equal volume of PBS in the same way.The doses (1mg/kg/i.p.) and the treatment regimen (every two days,start on day 5p.i.) are determined.

保存条件:
2-8℃
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

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

  • =
    *
    *
    *选择对应的单位 *空出希望得到的变量,填写另外两个变量

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 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    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):