EMD638683

产品编号: DC9620 Featured
EMD638683
结构式
1181770-72-8
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中国地区超过5000个高品质化合物库存
应用领域
EMD638683 是具有高度选择性的 SGK1 抑制剂,IC50 值为 3 μM。
Cas No.: 1181770-72-8
名称:
别名: EMD 638683;EMD-638683
SMILES: CC1=C(CC)C(C(NNC(C(O)C2=CC(F)=CC(F)=C2)=O)=O)=CC=C1O
分子式: C18H18F2N2O4
分子量: 364.3433
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: EMD638683 is a potent SGK1 inhibitor with an IC50 of 3 uM. The serum- and glucocorticoid-inducible kinase 1 (SGK1) is transcriptionally upregulated by mineralocorticoids and activated by insulin. EMD638683 could serve as a template for drugs 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. 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.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
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