Lixumistat (IM156)

製品コードS9604 バッチS960401

印刷

化学情報

Chemical Structure Synonyms HL156A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C13H16F3N5O
分子量 315.29 CAS No. 1422365-93-2
Solubility (25°C)* 体外 DMSO 63 mg/mL (199.81 mM)
Ethanol (warmed with 50ºC water bath) 20 mg/mL (63.43 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。

 4.000mg/ml (12.69mM) Taking the 1 mL working solution as an example, add 50 μL of 80 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。

 4.000mg/ml (12.69mM) Taking the 1 mL working solution as an example, add 50 μL of 80 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 Lixumistat (IM156), is a potent activator of AMPK that increases AMPK phosphorylation. IM156 blocks oxidative phosphorylation (OXPHOS) through the inhibition of complex I and increases apoptosis. IM156 ameliorates various types of fibrosis and inhibits tumors.
in vitro

Lixumistat (IM156) treatment of RPMCs inhibits HG-induced myofibroblast transdifferentiation and markers of epithelial-mesenchymal transition (EMT). Moreover, this compound ameliorates HG-induced transforming growth factor-β1, Smad3, Snail, and fibronectin expression in the RPMCs via AMPK upregulation.[3] It also decreases complex I-dependent NADH oxidation in a significant, dose-dependent manner.[2]
in vivo

In vivo treatment with Lixumistat (IM156) exacerbated the memory differentiation of virus-specific CD8+ T cells, resulting in an increase in short-lived effector cells but a decrease in memory precursor effector cells. Thus, this compound impairs the function of virus-specific memory CD8+ T cells, indicating that excessive AMPK activation weakens memory T cell differentiation, thereby suppressing recall immune responses.[1]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Rat peritoneal mesothelial cells (RPMCs)
濃度 10 μM, 30 μM, 50 μM
反応時間 24 h
実験の流れ

RPMCs are seeded at a density of 1 × 105 cells/well on a six-well plate. RPMCs are grown to 70% confluence and serum-starved under NG conditions for 24 h. The specific AMPKα1 small interfering (si)RNA, AMPKα2 siRNA, or control siRNA are transfected into the cells using a siRNA transfection reagent according to the manufacturer’s procedure. AMPKα1 siRNA, AMPKα2 siRNA, or control siRNA are incubated at final concentration of 20 μM using siRNA dilution buffer for 30 min at RT. The cells are washed twice with 2 ml of siRNA transfection medium, and 0.8 ml siRNA transfection medium and 200 μl siRNA transfection reagent complex are added to the well, covering the entire layer. The contents of the plate are gently mixed by swirling to ensure that the entire cell layer is immersed in the solution. Then, the cells are incubated for 5 h at 37°C in a 5% CO2 incubator. After that, 1 ml of normal growth medium is added. Next, the cells are incubated for an additional 24 h. Then, the media are replaced with fresh completed media and treated with NG or HG in the presence or absence of Lixumistat (IM156) for 24 h.
動物実験 動物モデル 5 to 6-wk-old female C57BL/6 mice
投薬量 5 mg/kg
投与方法 IP

参考

  • https://pubmed.ncbi.nlm.nih.gov/31089438/
  • https://pubmed.ncbi.nlm.nih.gov/32478334/
  • https://pubmed.ncbi.nlm.nih.gov/26661649/

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：

Therapeutic modulation of ROCK overcomes metabolic adaptation of cancer cells to OXPHOS inhibition and drives synergistic anti-tumor activity [ bioRxiv, 2024, 2024.09.16.613317] PubMed: 39345502

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。