受注:045-509-1970 |
技術サポート:[email protected] 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C18H18F2N2O4 |
|||
分子量 | 364.34 | CAS No. | 1181770-72-8 | |
Solubility (25°C)* | 体外 | DMSO | 73 mg/mL (200.36 mM) | |
Ethanol | 40 mg/mL (109.78 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | EMD638683 is a highly selective inhibitor of serum- and glucocorticoid-inducible kinase 1 (SGK1) with IC50 of 3 μM. EMD638683 exhibits antihypertensive potency and anti-tumor activity. |
---|---|
in vitro | In vitro testing discloses EMD638683 as a SGK1 inhibitor with an IC50 of 3 μM.[1] EMD638683 treatment significantly augments 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.[2] |
in vivo | The in vivo development of tumors following chemical carcinogenesis is significantly blunted by treatment with EMD638683.[2] Within 24 hours in vivo EMD638683 treatment significantly decreases blood pressure in fructose/saline-treated mice but not in control animals or in SGK1 knockout mice.[1] |
細胞アッセイ | 細胞株 | HeLa-cells |
---|---|---|
濃度 | 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM | |
反応時間 | 24 h | |
実験の流れ | The cells are plated in 6-wells MTPs at a density of 10–20 × 103 cells/cm2 in Dulbecco´s DMEM medium, supplemented with 10% fetal calf serum (FCS), 2 mM glutamine and 1 mM sodium pyruvate. After 24 hrs at 37℃ and 5% CO2 in a cell incubator, each well is further supplemented with 25 μl of a 100X dimethyl sulfoxide (DMSO) solution of the compound; the solution is diluted 100-fold in the supernatant of the cell culture, thus resulting in the anticipated SGK1-inhibitor concentration at a 1% DMSO concentration. |
|
動物実験 | 動物モデル | 8-week-old wild type mice |
投薬量 | 20 mg/kg, 600 mg/kg | |
投与方法 | IP, Oral gavage |
|
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。