Powder: -20°C for 3 years
In solvent: -80°C for 2 years
EMD638683,a novel SGK inhibitor with antihypertensive potency(with an IC50 of 3 μM).
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 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
DMSO: 50 mg/mL (137.23 mM)
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
EMD638683 1181770-72-8 代谢 SGK inhibit EMD-638683 Serum and glucocorticoid-regulated kinase EMD 638683 Inhibitor Serum-glucocorticoid regulated kinase inhibitor