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EMD638683

Catalog No. T6635 CAS 1181770-72-8

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

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EMD638683, CAS 1181770-72-8

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	EMD638683,a novel SGK inhibitor with antihypertensive potency(with an IC50 of 3 μM).
Targets&IC50	SGK1:3 μM
In vitro	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].
In vivo	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].
Cell Research	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].

Molecular Weight	364.349
Formula	C18H18F2N2O4
CAS No.	1181770-72-8

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 50 mg/mL (137.23 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Towhid S T , Liu G L , Ackermann T F , et al. Inhibition of Colonic Tumor Growth by the Selective SGK Inhibitor EMD638683[J]. Cellular Physiology and Biochemistry, 2013, 32(4):838-848. 2. Ackermann TF, Boini KM, Beier N,et al.EMD638683, a novel SGK inhibitor with antihypertensive potency[J].Cell Physiol Biochem. 2011;28(1):137-46.

Related compound libraries

This product is contained In the following compound libraries：

Glycometabolism Compound Library Anti-Cancer Metabolism Compound Library Inhibitor Library Anti-Metabolism Disease Compound Library Kinase Inhibitor Library Bioactive Compound Library

Related Products

Related compounds with same targets

SGK1-IN-4 SI-113 EMD638683 URMC-099 GSK 650394 AT13148 Ro-3306 CKI-7

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Keywords

EMD638683 1181770-72-8 代谢 SGK inhibit EMD-638683 Serum and glucocorticoid-regulated kinase EMD 638683 Inhibitor Serum-glucocorticoid regulated kinase inhibitor

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