Merck
CN
所有图片(1)

文件

JN0006

Sigma-Aldrich

Draflazine

≥98% (HPLC)

登录查看公司和协议定价
所有图片(1)
别名:
(-)-1-[2-(4-Amino-2,6-dichloro-anilino)-2-oxo-ethyl]-4-[5,5-bis(4-fluorophenyl)pentyl]piperazine-2-carboxamide, (-)-R 75,231, (-)-R 75231, (-)-R-75231, (-)-R75231, (S)-2-(Aminocarbonyl)-N-(4-amino-2,6-dichlorophenyl)-4-[5,5-bis(4-fluorophenyl)pentyl]-1-piperazineacetamide, (S)-R 75,231, (S)-R 75231, (S)-R-75231, (S)-R75231, R 88,021, R 88021, R-88021, R88021
经验公式（希尔记法）:
C30H33Cl2F2N5O2
CAS号:
138681-29-5
分子量:
604.52

检测方案

≥98% (HPLC)

形式

powder

旋光性

[α]/D -23 to -29°, c = 0.5 in ethanol

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

room temp

InChI

1S/C30H33Cl2F2N5O2/c31-25-15-23(35)16-26(32)29(25)37-28(40)18-39-14-13-38(17-27(39)30(36)41)12-2-1-3-24(19-4-8-21(33)9-5-19)20-6-10-22(34)11-7-20/h4-11,15-16,24,27H,1-3,12-14,17-18,35H2,(H2,36,41)(H,37,40)

InChI key

IWMYIWLIESDFRZ-UHFFFAOYSA-N

生化/生理作用

Draflazine (R88021; (-)-R75231), is a potent nucleoside transporter ENT1 (SLC29A1) inhibitor with 370-fold selectivity over ENT2 (SLC29A2). R88021 exhibits 30- and 40-times higher affinity as (+)-R75231 (R88016) using calf lung membrane preparation (by [3H]R75231 & [3H]NBI displacement) and intact human erythrocytes (by [3H]NBMPR displacement), respectively. Draflazine is 20-times more potent as R88016 in enhancing adenosine potency against ADP-induced aggregation in human whole blood (IC50 = 0.5 μM vs 10 μM with 1 μM respective inhibitor), Draflazine and R75231, but not R88016, show cardioprotective efficacy against catecholamines infusion in rabbits in vivo.

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

分析证书(COA)

输入产品批号来搜索 分析证书(COA) 。批号可以在产品标签上"批“ （Lot或Batch）字后找到。

已有该产品？

为方便起见，与您过往购买产品相关的文件已保存在文档库中。

访问文档库

难以找到您所需的产品或批次号码？

在网站页面上，产品编号会附带包装尺寸/数量一起显示（例如：T1503-25G）。请确保 在“产品编号”字段中仅输入产品编号 (示例: T1503).

示例

T1503
货号
-
25G
包装规格/数量

其它示例：

705578-5MG-PW

PL860-CGA/SHF-1EA

MMYOMAG-74K-13

1000309185

输入内容 1.000309185)

遇到问题？欢迎随时联系我们技术服务 寻求帮助

批号可以在产品标签上"批“ （Lot或Batch）字后面找到。

Aldrich 产品

  • 如果您查询到的批号为 TO09019TO 等，请输入去除前两位字母的批号：09019TO。

  • 如果您查询到的批号含有填充代码（例如05427ES-021），请输入去除填充代码-021的批号：05427ES。

  • 如果您查询到的批号含有填充代码（例如 STBB0728K9），请输入去除填充代码K9的批号：STBB0728。

未找到您寻找的产品？

部分情况下，可能未在线提供COA。如果搜索不到COA，可在线索取。

索取COA

H Van Belle et al.
Cardiovascular research, 27(1), 111-115 (1993-01-01)
R 75,231, a potent and specific nucleoside transport inhibitor, largely prevents cardiac damage and death in catecholamine challenged rabbits. The major biochemical effect of nucleoside transport inhibition in ischaemic and reperfused myocardium is a prolonged accumulation of adenosine. The cardioprotection
Nucleoside and nucleobase transport systems of mammalian cells.
D A Griffith et al.
Biochimica et biophysica acta, 1286(3), 153-181 (1996-10-29)
M W Beukers et al.
European journal of pharmacology, 266(1), 57-62 (1994-01-01)
In this study, we determined whether R75231, (+/-)-2-(aminocarbonyl)-N-(4-amino-2,6-dichlorophenyl)-4-[5,5-bis( 4-fluoro- phenyl)pentyl]-1-piperazineacetamide, and its two enantiomers, all nucleoside transport inhibitors, could play a role as anti-aggregatory agents. First, we determined the binding characteristics of [3H]nitrobenzylthioinosine, also a nucleoside transport inhibitor, on intact
J R Hammond
Naunyn-Schmiedeberg's archives of pharmacology, 361(4), 373-382 (2000-04-14)
The equilibrative nucleoside transporters of mammalian cells play an important role in the regulation of extracellular adenosine concentrations, and inhibition of these transporters potentiates the biological effects of adenosine. Two subtypes of equilibrative transporters have been defined by their differential
A P IJzerman et al.
Naunyn-Schmiedeberg's archives of pharmacology, 345(5), 558-563 (1992-05-01)
The tritiated analogue of R75231 ((+-)-2-(aminocarbonyl)-N-(4-amino-2,6-dichlorophenyl)-4-[5,5-bis (4-fluorophenyl)pentyl]-1-piperazineacetamide) has been examined as a new radioligand for (nitrobenzylthioinosine sensitive) nucleoside transport proteins. [3H]R75231 was prepared in two steps from R69064 ((+-)-4-[5,5-bis[4-fluorophenyl)-4-pentenyl]-2-piperazinecarboxamide+ ++ dihydrochloride) with a specific activity of 0.23 TBq/mmol (6.3 Ci/mmol).

我们的科学家团队拥有各种研究领域经验，包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.

联系技术服务部门