CDN1163

製品コードS6815 バッチS681501

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
化学式

C20H20N2O2

分子量 320.39 CAS No. 892711-75-0
Solubility (25°C)* 体外 DMSO 64 mg/mL (199.75 mM)
Ethanol 64 mg/mL (199.75 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 40%PEG300 5%Tween80 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。

2.500mg/ml (7.80mM) Taking the 1 mL working solution as an example, add 50 μL of 50 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 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。

5.000mg/ml (15.61mM) Taking the 1 mL working solution as an example, add 50 μL of 100 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 CDN1163 is a small molecular allosteric activator of the sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) that improves Ca2+ homeostasis.
in vitro

CDN1163 treatment significantly reduces the hepatic expression of genes involved in gluconeogenesis and lipogenesis, attenuates ER stress response and ER stress-induced apoptosis, and improves mitochondrial biogenesis, possibly through SERCA2-mediated activation of AMP-activated protein kinase pathway.[1]

in vivo

CDN1163 reduces blood glucose levels and improves metabolic parameters and gluconeogenic gene expression, reverses hepatic steatosis, inhibits ER stress and ER stress-induced apoptosis, and improves mitochondrial efficiency in ob/ob mice in vivo.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HEK cells
濃度 10 μm
反応時間 2 h
実験の流れ

Cells are grown in 96-well plates (n = 6) and exposed to CDN1163 (10 μm) or vehicle (DMSO) for 2 h followed by the addition of 200 μm H2O2 compared with untreated controls. H2O2 activates the unfolded protein response and is an inducer of ER stress-promoted apoptosis. After 16 h of incubation, cell viability is measured using Luminescent Cell Viability Assay.

動物実験 動物モデル Male 8-10-week old ob/ob mice and lean ob/+ mice
投薬量 50 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/26702054/

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:

SERCA-mediated endoplasmic reticulum stress facilitates hematopoietic stem cell mobilization [ Stem Cell Res Ther, 2025, 16(1):208] PubMed: 40275396
Proteome-wide CETSA reveals diverse apoptosis-inducing mechanisms converging on an initial apoptosis effector stage at the nuclear periphery [ Cell Rep, 2024, 43(10):114784] PubMed: 39365699
Aberrant miR-339-5p/neuronatin signaling causes prodromal neuronal calcium dyshomeostasis in mutant presenilin mice [ J Clin Invest, 2022, 132(8)e149160] PubMed: 35426376
Restoration of Sarco/Endoplasmic Reticulum Ca2+-ATPase Activity Functions as a Pivotal Therapeutic Target of Anti-Glutamate-Induced Excitotoxicity to Attenuate Endoplasmic Reticulum Ca2+ Depletion [ Front Pharmacol, 2022, 13:877175] PubMed: 35517826

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。