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CAS No.: 1181770-72-8

EMD638683 Catalog No. CSN17522

Synonyms: EMD638683

EMD638683 is a potent SGK1 inhibitor with an IC50 of 3 μM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述EMD638683 is a novel SGK Inhibitor with IC50 value of 3.35µM by determination of SGK1-dependent phosphorylation of NDRG1 (N-Myc downstream-regulated gene 1) in human cervical carcinoma HeLa-cells. Administration of EMD638683 (4460 ppm in chow, i.e. approx. 600mg/kg/day) to mice drinking tap water or isotonic saline containing 10% fructose significantly decreased blood pressure in fructose/saline-treated mice post 24h. It decreased blood pressure following chronic fructose/high salt treatment for 4 weeks. It abrogated the salt sensitivity of blood pressure in hyperinsulinism without appreciably affecting blood pressure in the absence of hyperinsulinism. Also EMD638683 tended to increase fluid intake and urinary excretion of Na⁺, significantly increased urinary flow rate and significantly decreased body weight. These suggested EMD638683 could serve as a template for drugs counteracting hypertension in individuals with type II diabetes and metabolic syndrome. In BMDMs primed with LPS, EMD638683 at 50μM ameliorated Ang II-stimulated IL-1β secretion in macrophages by blocking NLRP3 inflammasome activation post 8h. By reducing IL-1β production in macrophages, the transformation of fibroblasts to myofibroblasts was inhibited. This suggested the attenuation of Ang II-induced inflammation by EMD638683 may due to its inhibition of NLRP3 inflammasome/IL-1β secretion axis.
参考文献

[1] Towhid ST, Liu GL, et al. Inhibition of colonic tumor growth by the selective SGK inhibitor EMD638683. Cell Physiol Biochem. 2013;32(4):838-48.
[2] Ackermann TF, Boini KM, et al. EMD638683, a novel SGK inhibitor with antihypertensive potency. Cell Physiol Biochem. 2011;28(1):137-46.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7447 mL
- 13.7233 mL
- 27.4466 mL
- 5 mM
- 0.5489 mL
- 2.7447 mL
- 5.4893 mL
- 10 mM
- 0.2745 mL
- 1.3723 mL
- 2.7447 mL

技术信息

CAS号

1181770-72-8

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H18F2N2O4

运输

蓝冰

分子量

364.34

别名

EMD638683

溶解度

DMSO	180.0 mg/mL (494.0 mM)
Water	insoluble

动物实验配方

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