Phenformin HCl

製品コードS2542 バッチS254201

印刷

化学情報

Chemical Structure Synonyms NSC-756501, Phenethylbiguanide Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C10H15N5.HCl
分子量 241.72 CAS No. 834-28-6
Solubility (25°C)* 体外 DMSO 48 mg/mL (198.57 mM)
Water 48 mg/mL (198.57 mM)
Ethanol 12 mg/mL (49.64 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.
* <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 フェンホルミンHClは、ビグアナイド系の抗糖尿病薬であるフェンホルミンの塩酸塩です。これはAMPKを活性化し、その活性とリン酸化を増加させます。
in vitro

Phenformin stimulates the phosphorylation and activation of AMPKalpha1 and AMPKalpha2 without altering LKB1 activity. Phenformin increases AMPK activity and phosphorylation in the isolated heart, the increase in AMPK activity is always preceded by and correlated with increased cytosolic [AMP]. Phenformin is a 50-fold more potent inhibitor of mitochondrial complex I than 1,1-Dimethylbiguanide. Phenformin robustly induces apoptosis in LKB1 deficient NSCLC cell lines. Phenformin at 2 mM similarly induces AMPK signaling as shown by increased P-AMPK and P-Raptor levels. Phenformin induces higher levels of cellular stress, triggering induction of P-Ser51 eIF2α and its downstream target CHOP, and markers of apoptosis at later times. Phenformin induces a significant increase in survival and therapeutic response in KLluc mice following long-term treatment. Phenformin and AICAR increases AMPK activity in H441 cells in a dose-dependent fashion, stimulating the kinase maximally at 5-10 mm and 2 mm, respectively. Phenformin significantly decreases basal ion transport (measured as short circuit current) across H441 monolayers by approximately 50% compared with that of controls. Phenformin and AICAR significantly reduce MK-870-sensitive transepithelial Na+ transport compared with controls. Phenformin and AICAR suppress MK-870-sensitive Na+ transport across H441 cells via a pathway that includes activation of AMPK and inhibition of both apical Na+ entry through ENaC and basolateral Na+ extrusion via the Na+,K+-ATPase. Phenformin-treated rats reveals a tendency towards a decrease in blood insulin level (radioimmunoassay).

in vivo

Phenformin also increases levels of P-eIF2α and its target BiP/Grp78 in normal lung as well as in lung tumors of mice.

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/15068958/
  • https://pubmed.ncbi.nlm.nih.gov/17369473/
  • https://pubmed.ncbi.nlm.nih.gov/8496685/
  • https://pubmed.ncbi.nlm.nih.gov/15919715/
  • https://pubmed.ncbi.nlm.nih.gov/418748/

カスタマーフィードバック

Data from [Data independently produced by , , J Biol Chem, 2017, 292(7):2830-2841]

Data from [Data independently produced by , , Biochem Biophys Res Commun, 2016, 470(2):453-459]

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：

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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
Screening Health-Promoting Compounds for Their Capacity to Induce the Activity of FOXO3 [ J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493] PubMed: 34508571
Dietary Intake Regulates the Circulating Inflammatory Monocyte Pool [ cell, 2019, 178(5):1102-1114] PubMed: 31442403
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[ Oncotarget, 2017, ] PubMed: 28938614
Serine/Threonine Kinase Unc-51-like Kinase-1 (Ulk1) Phosphorylates the Co-chaperone Cell Division Cycle Protein 37 (Cdc37) and Thereby Disrupts the Stability of Cdc37 Client Proteins. [Li R, et al. J Biol Chem, 2017, 292(7):2830-2841] PubMed: 28073914
The epigenetic regulation of HIF-1α by SIRT1 in MPP(+) treated SH-SY5Y cells. [Dong SY, et al. Biochem Biophys Res Commun, 2016, 470(2):453-9] PubMed: 26768367

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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