中文名称: BAY 60-6583
英文名称: BAY 60-6583
CAS No: 910487-58-0
分子式: C19H17N5O2S
分子量: 379.44
B10826 BAY 60-6583 ≥98% (psaitong)
包装规格:
10mg in glass bottle
溶解性:
溶于DMSO(20mg/mL)
产品描述:

基本信息

产品编号:

B10826

产品名称:

BAY 60-6583

CAS:

910487-58-0

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C19H17N5O2S

溶于液体

-80℃

6个月

分子量:

379.44

-20℃

1个月

化学名: 

2-[6-amino-3,5-dicyano-4-[4-(cyclopropylmethoxy)phenyl]pyridin-2-yl]sulfanylacetamide

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

2.6355mL

13.1773mL

26.3546mL

5mM

0.5271mL

2.6355mL

5.2709mL

10mM

0.2635mL

1.3177mL

2.6355mL

 

生物活性

产品描述

一种腺苷A2B受体的高效选择性激动剂,对A2B受体 (EC50=3nM)的选择性高于A1,A2A和A3受体。BAY 60-6583可以与小鼠,兔和狗A2BAR 结合,Ki值分别为750nM,340nM和330 nM。BAY 60-6583在心肌缺血模型中具有心脏保护作用。

靶点

Adenosine Receptor

 

体外研究

BAY 60-6583 exhibits EC50 values for receptor activation >10,000nM for both A1 and A2A AR and 3nM for A2B AR subtype in CHO cells expressing recombinant human A1,A2A or A2B ARs.BAY 60-6583(0-10µM) exhibits the maximum agonist effect of BAY in the absence of siRNA is 68 %,which is significantly different from that in the presence of 5,50 and 500nM siRNA (54%,48% and 36%, respectively).It exhibits EC50  values of BAY in the absence and presence siRNA with 98±22,102±17,127±31 and 93±19nM,respectively,in T24 cells.BAY 60-6583 (5μM;24 hours) increases the accumulation of cells at the G1 phase with a decrease in G2/M phase in RAW264.7 preosteoclasts.BAY 60-6583 (5μM;24 hours) specifically inhibits the activation of Akt by M-CSF,whereas M-CSF-induced ERK1/2 activation is not affected by BAY 60-6583 treatment in RAW264.7 preosteoclasts.

Cell Cycle Analysis

Cell Line:

RAW264.7 preosteoclasts

Concentration:

5μM

Incubation Time:

48 hours

Result:

Caused an arrest of cells at the G1 phase.

Western Blot Analysis

Cell Line:

RAW264.7 preosteoclasts

Concentration:

5μM

Incubation Time:

48 hours

Result:

Exhibited an inhibition of M-CSF-mediated Akt activation and resulted in the decrease of osteoclast proliferation.

体内研究

BAY 60-6583 (intravenous injection;100 mcg/kg) reduces the infarction area just prior to reperfusion in ischaemic rabbit hearts.BAY 60-6583 (intraperitoneal injection;2mg/kg) attenuates LPS-induced lung injury,pre-treatment with this compound can significantly decrease LPS-increased IL-6 levels in WT-mice,In contrast,BAY 60-6583 treatment is ineffective in abrogating these inflammatory parameters in A2BAR−/− mice.BAY 60-6583 (intratumoral administration) causes a significant increase in tumor-infiltrating MDSCs,it does not affect neither their ability to suppress T-cell proliferation nor their degree of maturation,it also stimulates the production of IL-10 and CCL2 in the tumor tissue.

Animal Model:

A2BAR−/− mice on a C57BL/6J mice

Dosage:

2mg/kg

Administration:

Intraperitoneal injection;2mg/kg

Result:

Demonstrated attenuation of lung inflammation and pulmonary edema in wild-type but not in gene-targeted mice for the A2BAR.

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

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

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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

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  • 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):