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Merck
CN
所有图片(1)

主要文件

171261

Sigma-Aldrich

Dorsomorphin

≥95% (HPLC), liquid, AMPK inhibitor, Calbiochem

别名:

InSolution AMPK抑制剂,化合物C

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About This Item

经验公式(希尔记法):
C24H25N5O
分子量:
399.49
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77

产品名称

AMPK抑制剂,化合物C, InSolution, ≥95%, 10 mM, AMPK Inhibitor

质量水平

方案

≥95% (HPLC)

表单

liquid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
desiccated (hygroscopic)
protect from light

运输

wet ice

储存温度

2-8°C

SMILES字符串

[n]21ncc(c2ncc(c1)c4ccc(cc4)OCCN5CCCCC5)c3ccncc3

InChI

1S/C24H25N5O/c1-2-12-28(13-3-1)14-15-30-22-6-4-19(5-7-22)21-16-26-24-23(17-27-29(24)18-21)20-8-10-25-11-9-20/h4-11,16-18H,1-3,12-15H2

InChI key

XHBVYDAKJHETMP-UHFFFAOYSA-N

一般描述

一种细胞可透过性吡唑并嘧啶化合物,可抑制KDR/VEGFR2、ALK2/BMPR-1、AMPK激酶活性(IC50 = 25.1、148和234.6 nM),而对对ALK5/TGFβR-I、ZAPK、Syk、PKCθ、PKA或JAK3的作用却大大降低或几乎没有。研究表明,可阻断斑马鱼活体胚胎中BMP途径依赖性背腹发育(EC100 = 2.5 µ)和VEGF信号转导依赖性肌间血管形成(EC50 = 5 µM)。通常与 AMPK 激活剂 AICAR(货号 123040)和/或二甲双胍(货号 317240)结合使用,以研究 AMPK 依赖性细胞事件在体外和动物体内的生理反应。

生化/生理作用

主要靶标
AMPK
产物与ATP竞争。
可逆性:是
细胞可渗透性:具有
阻断斑马鱼活体胚胎中BMP途径依赖性背腹发育的EC100 = 2.5 µM;阻断VEGF信号转导依赖性肌间血管形成的EC50 = 5 µM
靶标IC50:抑制KDR/VEGFR2、ALK2/BMPR-1、AMPK激酶活性分别为25.1、148和234.6 nM

包装

用惰性气体包装

警告

毒性:刺激性(B)

外形

提供 10 mM(1 mg/250 µl)的 AMPK 抑制剂,化合物 C(货号171260),溶剂为DMSO

重悬

初次使用后,等分并冷冻(-20°C)。一旦打开,储备溶液在 -20°C 下可稳定保存 3 个月。

其他说明

Hao, J., et al. 2010.ACS Chem.Biol.5, 245.
Kim, E.K., et al. 2004.J. Biol. Chem.279, 19970.
Lee, M., et al. 2003.J. Biol. Chem.278, 39653.
Inoki, K., et al. 2003.Cell115, 577.
Fryer, L.G., 2002.FEBS Lett.531, 189.
Zhou, G., et al. 2001.J. Clin. Invest.108, 1167.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

储存分类代码

10 - Combustible liquids

WGK

WGK 2

闪点(°F)

188.6 °F - closed cup - (Dimethylsulfoxide)

闪点(°C)

87 °C - closed cup - (Dimethylsulfoxide)


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