EMD638683

製品コードS8824 バッチS882402

印刷

化学情報

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

73 mg/mL (200.36 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	3.650mg/ml (10.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 73 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.600mg/ml (1.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

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] This compound 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 this compound treatment significantly decreases blood pressure in fructose/saline-treated mice but not in control animals or in SGK1 knockout mice.^[1]

プロトコル(参考用のみ)

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 this 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

参考

https://pubmed.ncbi.nlm.nih.gov/21865856/
https://pubmed.ncbi.nlm.nih.gov/24081014/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Nedd4L signaling contributes to carbon tetrachloride-induced liver fibrosis in female mice and is associated with enteric dysbacteriosis [ Gastroenterol Rep (Oxf), 2025, 13:goaf022]	PubMed: 40066318

Nedd4L signaling contributes to carbon tetrachloride-induced liver fibrosis in female mice and is associated with enteric dysbacteriosis [ Gastroenterol Rep (Oxf), 2025, 13:goaf022]

PubMed: 40066318

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。