Metformin

製品コードS5958 バッチS595805

印刷

化学情報

 Chemical Structure Synonyms 1,1-Dimethylbiguanide Storage
(From the date of receipt)
3 years -20°C powder
化学式

C4H11N5

分子量 129.16 CAS No. 657-24-9
Solubility (25°C)* 体外 Water 130 mg/mL (1006.5 mM)
DMSO 26 mg/mL (201.3 mM)
Ethanol 26 mg/mL (201.3 mM)
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。

1.300mg/ml (10.07mM) Taking the 1 mL working solution as an example, add 50 μL of clarified DMSO stock solution of 26 mg/ml to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; 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. 
* <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 Metformin (1,1-Dimethylbiguanide), a widely used drug for treatment of type 2 diabetes, activates AMP-activated protein kinase (AMPK) in hepatocytes. Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.
in vitro

Metformin upregulates BAX activation with facilitation of BIM, BAD and PUMA, downregulates Bcl-2 and Bcl-xl, also induces cytochrome c release from mitochondria into the cytoplasm, directly triggering caspase-9-mediated mitochondrial apoptosis.[4]

in vivo

Metformin shows therapeutic effect of this compound in mouse model of liver fibrosis associated with nonalcoholic steatohepatitis (NASH) in which hepatic function, NASH lesions and fibrosis are improved.[4]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 human hepatic stellate cells (HSCs) LX-2, rat HSCs T6, human hepatocyte L02 and rat hepatocyte BRL-3A
濃度 0-80 mM
反応時間 24 h
実験の流れ

The human hepatic stellate cells (HSCs) LX-2 is maintained in RPMI 1640 medium, rat HSCs T6, human hepatocyte L02 and rat hepatocyte BRL-3A were maintained in DMEM, which are both supplemented with 10% (v/v) FBS and 1% (v/v) penicillin/streptomycin sulfate at 37 ℃ in a humidified 5% COincubator. Metformin and AICAR solutions are filtered through 0.22 μm millipore membrane filter units. CCK8 assay is used to detect the effects of different concentration of this compound and AICAR on the proliferation of hepatic stellate cells. T6 cells and LX-2 cells are treated with different concentration of this chemical and AICAR for 24 h, and the expression of collagen and α - SMA protein are detected by Western blot. Cells are treated with 10 mM this compound and 0.5 mM AICAR for 24 h, and the expression of collagen and α - SMA protein are detected by Western blot. The mRNA levels of collagen I and α - SMA are detected by RT-qPCR.

動物実験 動物モデル Male C57BL/6N mice
投薬量 10-200 mg/kg; 65 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/11602624/
  • https://pubmed.ncbi.nlm.nih.gov/31225649/
  • https://pubmed.ncbi.nlm.nih.gov/21895401/
  • https://pubmed.ncbi.nlm.nih.gov/35344814/

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Stromal Cell Derived Factor-1 Promotes Hepatic Insulin Resistance via Inhibiting Hepatocyte Lipophagy [ J Cell Mol Med, 2025, 29(2):e70352] PubMed: 39855896
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Metformin alleviates lung ischemia‑reperfusion injury via the SIRT1 pathway following lung transplantation in diabetic rats [ Mol Med Rep, 2025, 32(5)287] PubMed: 40808338
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Pump-Less, Recirculating Organ-On-Chip (rOoC) Platform To Model The Metabolic Crosstalk Between Islets and Liver [ Adv Healthc Mater, 2024, e2303785.] PubMed: 38221504

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。

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