1. Epigenetics
    PI3K/Akt/mTOR
    Autophagy
  2. AMPK
    Autophagy
  3. Phenformin hydrochloride

Phenformin hydrochloride (Synonyms: Phenethylbiguanide hydrochloride)

Cat. No.: HY-16397A Purity: 98.12%
Handling Instructions

Phenformin hydrochloride is an anti-diabetic drug from the biguanide class, can activate AMPK activity.

For research use only. We do not sell to patients.

Phenformin hydrochloride Chemical Structure

Phenformin hydrochloride Chemical Structure

CAS No. : 834-28-6

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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Phenformin hydrochloride purchased from MCE. Usage Cited in: Biomed Pharmacother. 2020 Aug;128:110216.

    Western blot analysis of p-AMPK, LC3B-I/II and NLRP3 after PSCs are pretreated with phenformin (Phe, AMPK activator) for 1 h followed by incubation with or without 10 μg/mL SSa for 24 h.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Phenformin hydrochloride is an anti-diabetic drug from the biguanide class, can activate AMPK activity.

    IC50 & Target[2]

    AMPK

     

    In Vitro

    Phenformin stimulates the phosphorylation and activation of AMPKalpha1 and AMPKalpha2 without altering LKB1 activity[1]. 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][2]. Phenformin is a 50-fold more potent inhibitor of mitochondrial complex I than metformin. 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[3]. 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 amiloride-sensitive transepithelial Na+ transport compared with controls. Phenformin and AICAR suppress amiloride-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[4]. Phenformin-treated rats reveals a tendency towards a decrease in blood insulin level (radioimmunoassay)[5].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Phenformin increases levels of P-eIF2α and its target BiP/Grp78 in normal lung as well as in lung tumors of mice[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    241.72

    Formula

    C₁₀H₁₆ClN₅

    CAS No.

    834-28-6

    SMILES

    NC(NC(NCCC1=CC=CC=C1)=N)=N.Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    H2O : 12.5 mg/mL (51.71 mM; Need ultrasonic)

    DMSO : 1 mg/mL (4.14 mM; ultrasonic and adjust pH to 2 with 1M HCl)

    Ethanol : < 1 mg/mL (insoluble)

    DMF : < 1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.1370 mL 20.6851 mL 41.3702 mL
    5 mM 0.8274 mL 4.1370 mL 8.2740 mL
    10 mM 0.4137 mL 2.0685 mL 4.1370 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 0.42 mg/mL (1.74 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 0.42 mg/mL (1.74 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 0.42 mg/mL (1.74 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Kinase Assay
    [2]

    Total AMPK activity is measured using the method of Dagher et al. AMPK activity is quantified in the resuspended pellet as incorporation of 32P from [γ-32P]ATP (10 GBq/mmol) into a synthetic peptide with the specific target sequence for AMPK, the SAMS peptide. Radioactivity is measured using a liquid scintillation counter. Protein content in the solution containing the resupended (NH4)2SO4 pellet is determined using the Bradford method.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 98.12%

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    Keywords:

    PhenforminPhenethylbiguanideAMPKAutophagyAMP-activated protein kinaseInhibitorinhibitorinhibit

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    Product Name:
    Phenformin hydrochloride
    Cat. No.:
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