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产品名称 EMD638683 英文名称 EMD638683 规格或纯度 98% 运输条件 超低温冰袋运输 生化机理 Description: IC50 Value: 3 μM EMD638683 is a SGK1 inhibitor.The serum- and glucocorticoid-inducible kinase 1 (SGK1) is transcriptionally upregulated by mineralocorticoids and activated by insulin. EMD638683 could serve as a template for drμgs counteracting hypertension in individuals with type II diabetes and metabolic syndrome. in vitro: EMD638683 was tested in vitro by determination of SGK1-dependent phosphorylation of NDRG1 (N-Myc downstream-regulated gene 1) in human cervical carcinoma HeLa-cells. EMD638683 was a SGK1 inhibitor with an IC50 of 3 μM[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[1]. Clinical trial:N/ACAS编号 1181770-72-8 溶解性 25°C: DMSO 储存温度 -20°C储存 分子量 364.34 分子式 C18H18F2N2O4 PubChem CID 44182398