Metformin HCl

For research use only.

Catalog No.S1950 Synonyms: 1,1-Dimethylbiguanide HCl

56 publications

Metformin HCl Chemical Structure

CAS No. 1115-70-4

Metformin HCl (1,1-Dimethylbiguanide HCl) decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis). Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.

Selleck's Metformin HCl has been cited by 56 publications

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Biological Activity

Description Metformin HCl (1,1-Dimethylbiguanide HCl) decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis). Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.
Targets
AMPK [1]
(Hepatocytes)
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 NIfF[lhHfW6ldHnvckBie3OjeR?= NV;lSoxMOSCvTR?= NVTzV3NxOjRiaB?= Mm[3RYN1cX[jdHnvckBw\iCDTWDLJIlvKGi3bXHuJGhmeEd{IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBodHWlb37lc4dmdmW|aYOgZZQhOSCvTTDh[pRmeiB{NDDodpMh[nliZX76fY1ifGmlIHPvcI9zcW2ndILpZ{Bie3OjeR?= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjR5MUC5NEc,OjZ2N{GwPVA9N2F-
mouse 3T3L1 cells MWXGeY5kfGmxbjDhd5NigQ>? M2P6UlEhdU1? NFjNNoFKdmS3Y4Tpc44hd2ZiQV3QT{BxcG:|cHjvdplt[XSrb36gbY4hdW:3c3WgN3Q{VDFiY3XscJMh[XRiMTDtUUBjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= M{m5[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkG2N|c6Lz5{NUKxOlM4QTxxYU6=
human HepG2 cells NE\BdldHfW6ldHnvckBie3OjeR?= NXLJXmFsOSCvTR?= NV:xNVRsOjRiaB?= NX7QVZRtWmWmdXP0bY9vKG:oIHfseYNwe2ViY3;ud5VueHSrb36gbY4hcW6|dXzpck1z\XOrc4ThcpQhcHWvYX6gTIVxTzJiY3XscJMh[XRiMTDtUUBi\nSncjCyOEBpenNiYomg[4x2[2:|ZTDvfIll[XOnIH3leIhw\CCrbjDwdoV{\W6lZTDv[kAzOi5{IH3NJI9nKGeudXPvd4U> M2fFfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEK1NlQ1Lz5{M{CyOVI1PDxxYU6=
human MDA-MB-231 cells NFLxemlHfW6ldHnvckBie3OjeR?= Mk\ONUB1dyB{MDDtUS=> NXHHcWR1OjRiaB?= NF3DblNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYYSgNUB1dyB{MDDtUUBi\nSncjCyOEBpenNiYomgUXRVKGG|c3H5Mi=> MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR3OUKwPEc,OjJ2NUmyNFg9N2F-
human HepG2 cells NWHGUnFCTnWwY4Tpc44h[XO|YYm= MlLZNlQhcA>? NVTkZm5{UW6lcnXhd4UhcW5iZ3z1Z49{\SClb37zeY1xfGmxbjDpckBqdnO3bHnuMZJme2m|dHHueEBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjCyOEBpenNuIFXDOVA:OC5{NzFOwG0v MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTh3NkC0PEc,OjF6NU[wOFg9N2F-
Hs575T NWP2WWh6TnWwY4Tpc44h[XO|YYm= M1nmSFIxKG2P M1Tp[lI1KGi{cx?= NFj5PI1KdmirYnn0bY9vKG:oIH3UU3IheGixc4Doc5J6dGG2aX;uJIlvKHS{aYDs[U1v\WejdHn2[UBpfW2jbjDId|U4PVRiY3XscJMh[XRiMkCgcW0h[W[2ZYKgNlQhcHK|IHL5JIludXWwb3Lsc5Qh[W6jbInzbZM> Ml2yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2OUCxOFgoRjJ|NEmwNVQ5RC:jPh?=
Hs578T M1;QZWFvfGmrbo\hd4l3\SCjc4PhfS=> M2jWbFIxKG2P NWDqbVlnOTdiaILz MUjBcpRqcW64YYPpeoUh[WO2aY\peJkh[WejaX7zeEB1emmybHWtcoVo[XSrdnWgbJVu[W5iSIO1O|hVKGOnbHzzJIF1KDJyIH3NJIFnfGW{IEG3JIhzeyCkeTDsbYdpfCCvaXPyc5Nkd3CrYzDhcoFtgXOrcx?= NWLSS2NVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0PVAyPDhpPkKzOFkxOTR6PD;hQi=>
Hs575T NF[3cpFHfW6ldHnvckBie3OjeR?= MXuyNEBuVQ>? Mkn3NlQhcHK| MX7BZ5RqfmG2aX;uJI9nKEGPUFugbY4hfHKrcHzlMY5m\2G2aY\lJIh2dWGwIFjzOVc2XCClZXzsd{BifCB{MDDtUUBi\nSncjCyOEBpenNiYomgbY1ufW6xYnzveEBidmGueYPpdy=> M1ywU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEmwNVQ5Lz5{M{S5NFE1QDxxYU6=
L6 NFzib3ZHfW6ldHnvckBie3OjeR?= NVX5ZplDOiCvTR?= NILZVmo1KGi{cx?= NHO4dXZKdmO{ZXHz[UBqdiCpbIXjc5NmKHWydHHr[UBqdiC{YYSgUFYh[2WubIOgZZQhOiCvTTD0doVifGWmIH\vdkA1KGi{czDwc5N1KDNyIH3pcpMhSU2SSzDpcohq[mm2b4KgZ49ueG:3bnSgR{B1emWjdH3lcpQ> M2jDUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUK4NVY{Lz5{OUGyPFE3OzxxYU6=
HepG2 NGTiRZRHfW6ldHnvckBie3OjeR?= NETsVmMyKG2P NYnvUYdKOjRiaILz MmHOTY5lfWO2aX;uJI9nKGeudXPvd4Uh[2:wc4XtdJRqd25iaX6gbJVu[W5iSHXwS|Ih[2WubIOgZZQhOSCvTTDpcoN2[mG2ZXSg[o9zKDJ2IHjydy=> NUi5cpVrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2OVE6QDRpPkK4OlUyQTh2PD;hQi=>

... Click to View More Cell Line Experimental Data
Assay
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
Immunofluorescence
LKB1; 

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.

26956973
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]

Protocol

Solubility (25°C)

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

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Chemical Information

Molecular Weight 165.62
Formula

C4H11N5.HCl
CAS No. 1115-70-4
Storage powder
in solvent
Synonyms 1,1-Dimethylbiguanide HCl
Smiles CN(C)C(=N)N=C(N)N.Cl

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04931017 Not yet recruiting Drug: Extended Release Metformin Hydrochloride Lung Carcinoma National Cancer Institute (NCI) November 1 2021 Phase 2
NCT04945148 Not yet recruiting Drug: Metformin|Radiation: Radiation IMRT|Drug: Temozolomide Glioblastoma IDH-wildtype Hopital Foch|National Cancer Institute France October 2021 Phase 2
NCT04169243 Not yet recruiting Behavioral: New Nordic Diet|Other: Control Gestational Diabetes Mellitus Göteborg University|Swedish Council for Working Life and Social Research October 2021 Not Applicable
NCT04530383 Not yet recruiting Drug: Metformin Hydrochloride Cystic Fibrosis-related Diabetes|Cystic Fibrosis University of Kansas Medical Center September 1 2021 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID