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EMD638683
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
EMD638683图片
CAS NO:1181770-72-8
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
EMD638683 是一种具有抗高血压效力的新型SGK抑制剂,IC50=3 μM。

产品描述

EMD638683,a novel SGK inhibitor with antihypertensive potency(with an IC50 of 3 μM).

体外活性

EMD638683 treatment significantly augmented the radiation-induced decrease of forward scatter, increase of phosphatidylserine exposure, decrease of mitochondrial potential, increase of caspase 3 activity, increase of DNA fragmentation and increase of late apoptosis. The in vivo development of tumors following chemical carcinogenesis was significantly blunted by treatment with EMD638683[1].

体内活性

Within 24 hours in vivo EMD638683 treatment significantly decreased blood pressure in fructose/saline-treated mice but not in control animals or in SGK1 knockout mice.?EMD638683 failed to alter the blood pressure in SGK1 knockout mice.?Following chronic (4 weeks) fructose/high salt treatment, additional EMD638683 treatment again decreased blood pressure.?EMD638683 thus abrogates the salt sensitivity of blood pressure in hyperinsulinism without appreciably affecting blood pressure in the absence of hyperinsulinism.?EMD638683 tended to increase fluid intake and urinary excretion of Na(+), significantly increased urinary flow rate and significantly decreased body weight[2].

细胞实验

Colon carcinoma (Caco-2) cells were exposed to EMD638683 with or without exposure to radiation (3 Gray) and cell volume was estimated from forward scatter, phosphatidylserine exposure from annexin V binding, mitochondrial potential from JC-9 fluorescence, caspase 3 activity from CaspGlow Fluorescein staining, DNA degradation from propidium iodide staining as well as late apoptosis from annexin-V FITC and propidium iodide double staining.?In vivo tumor growth was determined in wild type mice subjected to chemical carcinogenesis (intraperitoneal injection of 20 mg/kg 1,2-dimethylhydrazine followed by three cycles of 30 g/L synthetic dextran sulfate sodium in drinking water for 7 days)[1].

Cas No.

1181770-72-8

分子式

C18H18F2N2O4

分子量

364.349

储存和溶解度

DMSO:50 mg/mL (137.23 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years