Metformin HCl

For research use only. Not for use in humans.

Catalog No.S1950

15 publications

Metformin HCl  Chemical Structure

Molecular Weight(MW): 165.62

Metformin HCl decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis).

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Selleck's Metformin HCl has been cited by 15 publications

2 Customer Reviews

  • Cropped immunoblot analyses for downstream effector proteins of the MAPK and PI3K/AKT/mTOR signaling pathways for NRASQ61 mutant lung carcinoma and neuroblastoma cell lines. Dual pathway inhibition can be achieved by combining metformin and trametinib, as evidenced by the abolishment of p-ERK and p-S6.

    Oncotarget, 2015, 6(2): 969-78 . Metformin HCl purchased from Selleck.

  • Metformin added to atorvastatin therapy has no additional lipid-lowering effect. At the beginning of the experiment, rabbits were fed a high-cholesterol diet. After 2 weeks, rabbits were randomly stratified into the normal sodium (Ctrl group), atorvastatin (AT group), metformin (MT group), or atorvastatin/metformin combination therapy (AT + MT group) for a period of 10 weeks. Lipid levels were measured at −2, 0, 2, 6, 10 weeks after drug administration. Time-dependent changes and their AUC values of serum TC levels (A,B) are presented. Data are mean ± SD, n = 7 for each group. *P < 0.05, compared with Ctrl group. AUC, area under the curve; HDL-C, high-density lipoprotein cholesterol; LDL-C, low-density lipoprotein cholesterol; TC, total cholesterol.

    Sci Rep, 2017, 7(1):2169. Metformin HCl purchased from Selleck.

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Biological Activity

Description Metformin HCl decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis).
AMPK [1]
In vitro

Metformin (500 μM) activates AMPK in hepatocytes, as a result, acetyl-CoA carboxylase (ACC) activity is reduced, fatty acid oxidation is induced, and expression of lipogenic enzymes is suppressed. Metformin (2 mM) activates muscle AMPK and promotes glucose uptake. Metformin (500 μM) or AICAR strongly suppresses SREBP-1 mRNA expression in rat hepatocytes. Metformin ameliorates hyperglycemia without stimulating insulin secretion, promoting weight gain, or causing hypoglycemia. Metformin has beneficial effects on circulating lipids linked to increased cardiovascular risk. Metformin decreases hepatic glucose production and increases skeletal myocyte glucose uptake. [1] Metformin requires LKB1 in the liver to lower blood glucose levels. [2] Metformin (2 mM) leads to a significant increase in the activity of both α1- and α2-containing complexes in muscle cells. Metformin (2 mM) also increases threonine 172 phosphorylation in muscle cells. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HepG2 cells MlfiSpVv[3Srb36gZZN{[Xl? MWqyOEBp NYryZlhmUW6lcnXhd4UhcW5iZ3z1Z49{\SClb37zeY1xfGmxbjDpckBqdnO3bHnuMZJme2m|dHHueEBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjCyOEBpenNuIFXDOVA:OC5{NzFOwG0v Mm\DNlE5PTZyNEi=
human MDA-MB-231 cells M17HZWZ2dmO2aX;uJIF{e2G7 MUKxJJRwKDJyIH3N NXrmT|ZNOjRiaB?= M1:3WWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjdDCxJJRwKDJyIH3NJIFnfGW{IEK0JIhzeyCkeTDNWHQh[XO|YYmu NWnQXGlWOjJ2NUmyNFg>
human HepG2 cells MYXGeY5kfGmxbjDhd5NigQ>? MVqxJI1O NVTO[XlyOjRiaB?= MWXS[YR2[3Srb36gc4Yh\2y3Y3;z[UBkd26|dX3weIlwdiCrbjDpcpN2dGmwLYLld4l{fGGwdDDoeY1idiCKZYDHNkBk\WyuczDheEAyKG2PIHHmeIVzKDJ2IHjyd{BjgSCpbIXjc5NmKG:6aXThd4UhdWW2aH;kJIlvKHC{ZYPlcoNmKG:oIEKyMlIhdU1ib3[g[4x2[2:|ZR?= NHr3e2QzOzB{NUK0OC=>
mouse 3T3L1 cells NXTWfZBETnWwY4Tpc44h[XO|YYm= NW\5W29sOSCvTR?= MVnJcoR2[3Srb36gc4YhSU2SSzDwbI9{eGixconsZZRqd25iaX6gcY92e2ViM2SzUFEh[2WubIOgZZQhOSCvTTDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? NYjTcGVZOjV{MU[zO|k>
human HepG2 cells NHfDS2hHfW6ldHnvckBie3OjeR?= NIXmcY8yKG2P MojsNlQhcA>? MX;BZ5RqfmG2aX;uJI9nKEGPUFugbY4hcHWvYX6gTIVxTzJiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJIdtfWOxbnXv[4Vv\XOrczDheEAyKG2PIHHmeIVzKDJ2IHjyd{BjgSCnbor5cYF1cWNiY3;sc5JqdWW2cnnjJIF{e2G7 M1vidVI3PDdzMEmw

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p-AMPK / AMPK / p-mTOR / mTOR / p-S6K / S6K; 

PubMed: 24505341     

The combined effects of metformin and heating were studied by heating the cells at 39.5–41°C for 1 h with 5 mM metformin and then incubating at 37°C for 47 h.

TTP / p-STAT3 / STAT3 / c-Myc ; 

PubMed: 26956973     

Metformin treatment increases phospho-AMPK (pAMPK) but decreases c-Myc and phospho-STAT3 (pSTAT3) in MCF7 and MDA-MB-231 cells. MCF7 and MDA-MB-231 cells were treated with 6 mM metformin for the indicated length of time, and the levels of TTP, STAT3, pSTAT3, AMPK, pAMPK, and c-Myc were measured by Western blotting.

pACC / ACC / pS6 / S6; 

PubMed: 26172303     

Western blot of pACC Ser79 (280 kDa), ACC (265 kDa), pS6 Ser240/244 (32 kDa), S6 (32 kDa), and β-actin (42 kDa) in HeyA8 cells treated with 0-5 mM metformin in normoglycemic or hyperglycemic conditions for 24 h.

pSTAT3 (Ser727) / STAT3 / Jak2 / Cdk5 / pNFκB / Bcl-2 / Bcl-XL / c-Myc; 

PubMed: 28114390     

Western blot of STAT3 and its regulatory proteins in Ishikawa cells after treatment with control, 10 mM, or 20 mM metformin for 48h in high-glucose conditions.

24505341 26956973 26172303 28114390

PubMed: 29601127     

LKB1 location with or without 10 lmol/L metformin treatment in Capan-2 wtLKB1 cell line. Scale bar, 50 μm.

PAR ; 

PubMed: 21422199     

A. MCF7 (left panel) or MDA-MB-231 (right panel) cells were treated with (Met) or without (Con) metformin for 2.5 days and then PAR (red) was detected by immunofluorescence using confocal microscopy. Nuclei (blue) were stained with DAPI.

CD86 / CD206; 

PubMed: 30899369     

Representative images of immunofluorescence analysis of macrophage phenotype in vitro, CD86 (M1 green) or CD206 (M2 red) were analysis. Scale bar 50 μm.

beta-catenin / AMPK; 

PubMed: 30854043     

Cells were treated with metformin for 24 h and subjected to immunofluorescence staining for β-catenin and AMPK. Magnification, ×400.

29601127 21422199 30899369 30854043
Growth inhibition assay
Cell viability ; 

PubMed: 26956973     

MCF7 and MDA-MB-231 cells were treated with the indicated concentrations of metformin for 24 h. Cell viability was assessed by measuring absorbance at 490 nm using an MTS cell proliferation assay. The values obtained with mock-treated cells were set to 100. Values are the mean ± SD (n = 3). *p < 0.05, **p < 0.01, ***p < 0.001.

In vivo Metformin (100 mg/ml, po) treatment produces significant decreases in hepatic expression of mRNAs for SREBP-1, FAS, and S14 in SD rats that are consistent with effects documented in cells. Metformin also decreases hepatic lipids in obese mice. [1] Metformin (250 mg/kg, i.p.) increases AMPK phosphorylation in livers of wild-type mice. Metformin (250 mg/kg, i.p.) treatment reduces blood glucose by more than 50% in the wild-type mice on a high-fat diet. Metformin (250 mg/kg, i.p.) treatment also loweres blood glucose in the ob/ob mice by 40%. [2]


Solubility (25°C)

In vitro Water 33 mg/mL warmed (199.25 mM)
DMSO Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 165.62


CAS No. 1115-70-4
Storage powder
in solvent
Synonyms N/A
Smiles Cl.CN(C)C(=N)NC(N)=N

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03416127 Not yet recruiting Drug: Propolis|Drug: Metformin|Drug: Placebo Diabetes Mellitus Type 2 University of Guadalajara October 30 2019 Phase 2
NCT03710343 Not yet recruiting Drug: Metformin|Drug: Placebo Oral Tablet Cerebral Palsy|Spastic|Spastic Cerebral Palsy|Cerebral Palsy Spastic|Cerebral Palsy Mixed Holland Bloorview Kids Rehabilitation Hospital|The Hospital for Sick Children September 1 2019 Phase 2
NCT03994744 Recruiting Drug: PD-1 inhibitor|Drug: Metformin Small-cell Lung Cancer|Small Cell Lung Carcinoma|Small Cell Lung Cancer Recurrent|Small Cell Lung Cancer Extensive Stage Hunan Cancer Hospital|Xiangya Hospital of Central South University|Innovent Biologics (Suzhou) Co. Ltd. August 20 2019 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID