2. Epigenetics PI3K/Akt/mTOR Autophagy Apoptosis
  3. AMPK Autophagy Mitophagy Apoptosis mTOR
  4. Metformin

Metformin  (Synonyms: 1,1-Dimethylbiguanide)

Cat. No.: HY-B0627 Purity: 99.96%
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Metformin (1,1-Dimethylbiguanide) inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo.

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

Metformin Chemical Structure

Metformin Chemical Structure

CAS No. : 657-24-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
Solid
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Based on 145 publication(s) in Google Scholar

Other Forms of Metformin:

Metformin Related Antibodies

Top Publications Citing Use of Products

132 Publications Citing Use of MCE Metformin

WB
IHC
Cell Viability Assay

    Metformin purchased from MedChemExpress. Usage Cited in: Redox Biol. 2023 Jun 15, 102786.

    Metformin hydrochloride (Metformin; 2, 6, 20 mM; 30 min) attenuates MGO-induced cell death in a concentration-dependent manner in ARPE-19 cells.

    Metformin purchased from MedChemExpress. Usage Cited in: Redox Biol. 2023 Jun 15, 102786.

    Metformin hydrochloride (Met; 3, 6 mM; 30 min) inhibits MGO-induced the increased expression of Bax and caspase-3 cleavage and decreased expression of Bcl-2 in ARPE-19 cells.

    Metformin purchased from MedChemExpress. Usage Cited in: Endocrinology. 2018 May 1;159(5):2008-2021.  [Abstract]

    Male C57BL/6 mice are intragastrically treated with Metformin or placebo at 3 mg/kg/day for 10 weeks in the presence of HFD after 10-week-HFD feeding and then sacrificed for sample collection. Western blot analysis of AMPKα1, AMPK, p-AMPK, SREBP1 and FAS.

    Metformin purchased from MedChemExpress. Usage Cited in: Mol Cell Proteomics. 2017 Jul;16(7):1324-1334.  [Abstract]

    To further validate the MS quantification results, Western blot analysis is carried out using an anti-H3K36 dimethylation antibody. Consistent with the mass spectrometric data, H3K36 dimethylation was elevated in DIO mouse livers, whereas Metformin treatment can significantly decrease histone H3K36 dimethylation in DIO mice to a level close to that of the chow-fed control mice.

    Metformin purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049.  [Abstract]

    Co-treatment of Metformin and Ribociclib induces cell death in Hep3B cells. Cells are exposed to Ribociclib at 25 μM and/or Metformin at 10 mM for 72 h.

    Metformin purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2017 Oct;11(10):1475-1492.  [Abstract]

    (A) IHC staining of N-cadherin and E-cadherin in the pancreas from KPC mice treated with vehicle, Metformin, or KRIBB11. (B) Masson's trichrome staining and IHC staining of α-SMA in pancreatic tissues from mice treated with vehicle, Metformin, or KRIBB11.

    Metformin purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2017 Oct;11(10):1475-1492.  [Abstract]

    MiaPaCa-2 cells are treated with a gradient concentration of Metformin for 24 h, and then, western blotting is performed to show the activation of p-AMPK and the suppression of HSF1 and HSP70.

    Metformin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2017 Aug 15;138:49-60.  [Abstract]

    PP5 overexpression suppresses AMPK-Thr172 phosphorylation induced by AMPK activators, AICAR and metformin. Hep3B cells are transfected with indicated plasmids and treated with AICAR (2 mM; 3 h) or Metformin (3 mM; 16 h) to simulate AMPK phosphorylation.

    Metformin purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2017 Dec;21(12):3322-3336.  [Abstract]

    Metformin prevents the loss of tight junction (TJ) proteins after SCI. Representative Western blots and quantification data of Occludin, Claudin-5, ZO-1 and β-actin at 3 day after injury.

    Metformin purchased from MedChemExpress. Usage Cited in: Mol Neurobiol. 2017 Jul;54(5):3327-3341.  [Abstract]

    Met attenuates apoptosis caused by traumatic spinal cord injury in rat. a, b Representative western blots and quantification data of cleaved caspase 3 and β-actin in each group rats. c, d Representative western blots and quantification data of Bax, Bcl-2, and β-actin in each group rats.

    Metformin purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2017;44(4):1381-1395.  [Abstract]

    U87 cells are treated with Met alone or in the presence of isogambogenic acid for 24 h. The expression levels of phosphorylated AMPK, mTOR and 4E-BP1 are assessed by western blotting, with total AMPK, mTOR and 4E-BP1 used as the internal controls.

    Metformin purchased from MedChemExpress. Usage Cited in: Front Immunol. 2016 Dec 12;7:597.  [Abstract]

    Metformin increases adenosine triphosphate-induced inflammasome activation in bone marrow-derived macrophages. (A) Cells are treated. Indicated protein levels in both cell lysates and supernatants are evaluated by western blotting. β-Tubulin is used as a loading control for cell lysates. (B–D) The quantitative analyses of the active caspase-1p10 (B), mature interleukin-1β (C), and HMGB1 (D) levels in the supernatants (A) are shown.

    Metformin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2016 Oct 20;7:390.  [Abstract]

    Metformin, an AMPK agonist, counteracts the effect of Piperine on suppressing ATP-induced AMPK activation and inflammatory mediator release. J774A.1 cells are pre-treated with 80 μM Piperine and BMDMs are pre-treated with 160 μM Piperine for 4 h. Without being washed out of Piperine, these cells are primed with LPS (500 ng/mL) for 4 h. Next, the cells are treated with Metformin (1 mM) for 1 h (in the absence of Piperine and LPS). Finally, in the presence of Metformin, the BMDMs are stimulated wi

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    • Biological Activity

    • Purity & Documentation

    • References

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    Description

    Metformin (1,1-Dimethylbiguanide) inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo[1][2][3][4][5][6][7].

    IC50 & Target[1]

    AMPK

     

    In Vitro

    Metformin (1,1-Dimethylbiguanide) inhibits proliferation of ESCs in a concentration-dependent manner. The IC50 is 2.45 mM for A-ESCs and 7.87 mM for N-ESCs. Metformin shows pronounced effects on activation of AMPK signaling in A-ESCs from secretory phase than in cells from proliferative phase[3].
    Metformin (0-500 μM) decreases glycogen synthesis in a dose-dependent manner with an IC50 value of 196.5 μM in cultured rat hepatocytes[4].
    Metformin shows cell viability and cytotoxic effects on PC-3 cells with IC50 of 5 mM[5].
    Metformin (1–50 mM; 0-120 h) significantly inhibites the proliferation of both 786-O and OS-RC-2 RCC cell lines in a dose- and time-dependent manner[7].
    Metformin (5 mM; 0-48 h) stimulates AMPK and inhibited the mTOR signaling pathway in 786-O cells[7].

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

    Metformin Related Antibodies

    Cell Proliferation Assay[7]

    Cell Line: 786-O and OS-RC-2 cells
    Concentration: 1、5、10、20 and 50 mM
    Incubation Time: 0-120 h
    Result: Inhibited the growth of 786-O and OS-RC-2 cells by 10% and 14% at doses of 0.2 and 0.5 mM, respectively.

    Western Blot Analysis[7]

    Cell Line: 786-O cells
    Concentration: 5 mM
    Incubation Time: 0-48 h
    Result: Reduced phosphorylation of S6K1 (Thr389) in a time-dependent manner, and thus reduced phosphorylation of ribosomal S6 protein (Ser235/236).
    Activated AMPK in a time-dependent manner.
    In Vivo

    Metformin (1,1-Dimethylbiguanide; 100 mg/kg, p.o.) alone, and metformin (25, 50, 100 mg/kg) with isoproterenol groups attenuates myocyte necrosis through histopathological analysis[1].
    Metformin (> 900 mg/kg/day, p.o.) results in moribundity/mortality and clinical signs of toxicity in Crl:CD(SD) rats[2].
    Metformin (200 mg/kg; i.p.; once a day for 6 consecutive days before induction of ischemia and at the beginning of reperfusion) significantly reduces the serum alanine aminotransferase (ALT) level in rats with ischemia-reperfusion model[6].
    Metformin (250 mg/kg; i.p.; once daily for 22 days) significantly reduces the growth of 786-O cell xenograft tumors in nude mice[7].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    129.17

    Formula

    C4H11N5
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    NC(NC(N(C)C)=N)=N
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    -20°C, protect from light, stored under nitrogen

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

    Solvent & Solubility
    In Vitro: 

    H2O : 50 mg/mL (387.10 mM; Need ultrasonic)

    DMSO : 25 mg/mL (193.55 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 7.7419 mL 38.7096 mL 77.4192 mL
    5 mM 1.5484 mL 7.7419 mL 15.4838 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: ≥ 2.08 mg/mL (16.10 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: ≥ 2.08 mg/mL (16.10 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 100 mg/mL (774.19 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.98%

    SDS (393 KB)

    COA (243 KB) HNMR (141 KB) RP-HPLC (168 KB) LCMS (104 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 7.7419 mL 38.7096 mL 77.4192 mL 193.5479 mL
    5 mM 1.5484 mL 7.7419 mL 15.4838 mL 38.7096 mL
    10 mM 0.7742 mL 3.8710 mL 7.7419 mL 19.3548 mL
    15 mM 0.5161 mL 2.5806 mL 5.1613 mL 12.9032 mL
    20 mM 0.3871 mL 1.9355 mL 3.8710 mL 9.6774 mL
    25 mM 0.3097 mL 1.5484 mL 3.0968 mL 7.7419 mL
    30 mM 0.2581 mL 1.2903 mL 2.5806 mL 6.4516 mL
    40 mM 0.1935 mL 0.9677 mL 1.9355 mL 4.8387 mL
    50 mM 0.1548 mL 0.7742 mL 1.5484 mL 3.8710 mL
    60 mM 0.1290 mL 0.6452 mL 1.2903 mL 3.2258 mL
    80 mM 0.0968 mL 0.4839 mL 0.9677 mL 2.4193 mL
    100 mM 0.0774 mL 0.3871 mL 0.7742 mL 1.9355 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Metformin Related Classifications

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Metformin657-24-91,1-DimethylbiguanideAMPKAutophagyMitophagyApoptosismTORAMP-activated protein kinaseMitochondrial AutophagyMammalian target of Rapamycinmitochondrialrespiratorychainliverinsulinsensitivitytype2diabetesblood-brainbarrierInhibitorinhibitorinhibit

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