Metformin HCl

For research use only.

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

49 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.

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Selleck's Metformin HCl has been cited by 49 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 Mkj3SpVv[3Srb36gZZN{[Xl? NGS0TVQyKG2P NIXZ[HgzPCCq NHTF[FJC[3SrdnH0bY9vKG:oIFHNVGshcW5iaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKGeudXPvcoVw\2WwZYPpd{BifCBzIH3NJIFnfGW{IEK0JIhzeyCkeTDlcpp6dWG2aXOgZ49td3KrbXX0dolkKGG|c3H5 M{fGcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NEexNFkxLz5{NkS3NVA6ODxxYU6=
mouse 3T3L1 cells NFnBVIRHfW6ldHnvckBie3OjeR?= M{PYZ|EhdU1? NWKz[YVbUW6mdXP0bY9vKG:oIFHNVGsheGixc4Doc5J6dGG2aX;uJIlvKG2xdYPlJFNVO0xzIHPlcIx{KGG2IEGgcW0h[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz MlfuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MU[zO|koRjJ3MkG2N|c6RC:jPh?=
human HepG2 cells NGntdndHfW6ldHnvckBie3OjeR?= NV6wZW5uOSCvTR?= MXeyOEBp M3[xcnJm\HWldHnvckBw\iCpbIXjc5NmKGOxboP1cZB1cW:wIHnuJIlve3WuaX6tdoV{cXO2YX70JIh2dWGwIFjldGczKGOnbHzzJIF1KDFibV2gZYZ1\XJiMkSgbJJ{KGK7IHfseYNwe2Vib4jp[IF{\SCvZYToc4QhcW5icILld4Vv[2Vib3[gNlIvOiCvTTDv[kBodHWlb4Pl NHLFb5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{CyOVI1PCd-MkOwNlUzPDR:L3G+
human MDA-MB-231 cells Ml;YSpVv[3Srb36gZZN{[Xl? MkfONUB1dyB{MDDtUS=> MlW2NlQhcA>? MnjnRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGG2IEGgeI8hOjBibV2gZYZ1\XJiMkSgbJJ{KGK7IF3UWEBie3OjeT6= NF[4RpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkS1PVIxQCd-MkK0OVkzODh:L3G+
human HepG2 cells MkCxSpVv[3Srb36gZZN{[Xl? MmCxNlQhcA>? NYLjOWYxUW6lcnXhd4UhcW5iZ3z1Z49{\SClb37zeY1xfGmxbjDpckBqdnO3bHnuMZJme2m|dHHueEBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjCyOEBpenNuIFXDOVA:OC5{NzFOwG0v NFXWWm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUi1OlA1QCd-MkG4OVYxPDh:L3G+
Hs575T NGC4[2xHfW6ldHnvckBie3OjeR?= NImxN4szOCCvTR?= M{XJflI1KGi{cx?= M3;KT2lvcGmkaYTpc44hd2ZibWTPVkBxcG:|cHjvdplt[XSrb36gbY4hfHKrcHzlMY5m\2G2aY\lJIh2dWGwIFjzOVc2XCClZXzsd{BifCB{MDDtUUBi\nSncjCyOEBpenNiYomgbY1ufW6xYnzveEBidmGueYPpdy=> MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR7MEG0PEc,OjN2OUCxOFg9N2F-
Hs578T MUTBcpRqcW64YYPpeoUh[XO|YYm= M{PUT|IxKG2P NIDycG0yPyCqcoO= NXHlWm1SSW62aXnueoF{cX[nIHHjeIl3cXS7IHHnZYlve3RidILpdIxmNW6nZ3H0bZZmKGi3bXHuJGh{PTd6VDDj[YxteyCjdDCyNEBuVSCjZoTldkAyPyCqcoOgZpkhdGmpaISgcYlkem:|Y3;wbYMh[W6jbInzbZM> MkTNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2OUCxOFgoRjJ|NEmwNVQ5RC:jPh?=
Hs575T MX3GeY5kfGmxbjDhd5NigQ>? NHvaPIYzOCCvTR?= MWmyOEBpenN? NEniS5hC[3SrdnH0bY9vKG:oIFHNVGshcW5idILpdIxmNW6nZ3H0bZZmKGi3bXHuJGh{PTd3VDDj[YxteyCjdDCyNEBuVSCjZoTldkAzPCCqcoOgZpkhcW2vdX7vZoxwfCCjbnHsfZNqew>? MlnsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2OUCxOFgoRjJ|NEmwNVQ5RC:jPh?=
L6 NYPmbIRWTnWwY4Tpc44h[XO|YYm= MkHoNkBuVQ>? NHv3c441KGi{cx?= M4m1eGlv[3KnYYPlJIlvKGeudXPvd4UhfXC2YXvlJIlvKHKjdDDMOkBk\WyuczDheEAzKG2PIITy[YF1\WRiZn;yJFQhcHK|IIDvd5QhOzBibXnud{BCVVCNIHnubIljcXSxcjDjc41xd3WwZDDDJJRz\WG2bXXueC=> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF{OEG2N{c,OjlzMkixOlM9N2F-
HepG2 NE\JVHFHfW6ldHnvckBie3OjeR?= NF[xUIQyKG2P Mn\aNlQhcHK| MkWyTY5lfWO2aX;uJI9nKGeudXPvd4Uh[2:wc4XtdJRqd25iaX6gbJVu[W5iSHXwS|Ih[2WubIOgZZQhOSCvTTDpcoN2[mG2ZXSg[o9zKDJ2IHjydy=> NI\BXZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[1NVk5PCd-Mki2OVE6QDR:L3G+

... 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
NCT04758000 Recruiting Drug: Metformin Hydrochloride Osteosarcoma|Ewing Sarcoma Istituto Ortopedico Rizzoli March 1 2021 Phase 2
NCT04583462 Not yet recruiting Drug: Metformin|Drug: Placebo Peripheral Arterial Calcification in Type 1 Diabetes Assistance Publique - Hôpitaux de Paris December 1 2020 Phase 3
NCT02978547 Unknown status Drug: Metformin Hydrochloride 500Mg Tablet Resectable Pancreatic Ductal Adenocarcinoma British Columbia Cancer Agency|Pancreatic Cancer Canada|BC Cancer Foundation January 2019 Phase 2
NCT03722290 Completed Drug: Metformin Fragile X Syndrome Université de Sherbrooke|FRAXA Research Foundation September 1 2018 Phase 2
NCT02684578 Recruiting Drug: Metformin Age-Related Macular Degeneration|Macular Degeneration Age-Related|Dry Macular Degeneration|Geographic Atrophy University of California San Francisco|San Francisco Veterans Affairs Medical Center|VA Palo Alto Health Care System|University of California Davis|University of California Los Angeles|University of California Irvine|University of California San Diego|Northwestern University|University of Illinois at Chicago|Retinal Consultants Medical Group|Retina Health Center|California Retina Consultants|Oregon Health and Science University April 2016 Phase 2
NCT03361878 Completed Drug: Metformin Hydrochloride Diabetes Mellitus Type 2|Metformin Adverse Reaction NHS Tayside|University of Southern Denmark|University of Dundee|Helmholtz Zentrum München May 4 2014 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID