Metformin HCl

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

For research use only.

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.

Metformin HCl  Chemical Structure

CAS No. 1115-70-4

Selleck's Metformin HCl has been cited by 61 publications

Purity & Quality Control

Choose Selective Carbohydrate Metabolism Inhibitors

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 NWrPc|lbTnWwY4Tpc44h[XO|YYm= MVixJI1O NHjnblQzPCCq NYjPW2d1SWO2aY\heIlwdiCxZjDBUXBMKGmwIHj1cYFvKEincFeyJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iCpbIXjc45md2enbnXzbZMh[XRiMTDtUUBi\nSncjCyOEBpenNiYomg[Y57gW2jdHnjJINwdG:{aX3leJJq[yCjc4PhfS=> MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjR5MUC5NEc,OjZ2N{GwPVA9N2F-
mouse 3T3L1 cells M1niN2Z2dmO2aX;uJIF{e2G7 NV;aZ2hwOSCvTR?= NFHOcm5KdmS3Y4Tpc44hd2ZiQV3QT{BxcG:|cHjvdplt[XSrb36gbY4hdW:3c3WgN3Q{VDFiY3XscJMh[XRiMTDtUUBjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= NWjpVGl{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVY{PzlpPkK1NlE3Ozd7PD;hQi=>
human HepG2 cells NXrUfWU1TnWwY4Tpc44h[XO|YYm= NFTNTHIyKG2P M3X1dVI1KGh? NF;MNGFT\WS3Y4Tpc44hd2ZiZ3z1Z49{\SClb37zeY1xfGmxbjDpckBqdnO3bHnuMZJme2m|dHHueEBpfW2jbjDI[ZBIOiClZXzsd{BifCBzIH3NJIFnfGW{IEK0JIhzeyCkeTDncJVkd3OnIH;4bYRie2VibXX0bI9lKGmwIIDy[ZNmdmOnIH;mJFIzNjJibV2gc4Yh\2y3Y3;z[S=> M2nMN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEK1NlQ1Lz5{M{CyOVI1PDxxYU6=
human MDA-MB-231 cells M4P6d2Z2dmO2aX;uJIF{e2G7 NIWxfYgyKHSxIEKwJI1O MlPUNlQhcA>? NVH4fI13SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHH0JFEhfG9iMkCgcW0h[W[2ZYKgNlQhcHK|IHL5JG1VXCCjc4PhfU4> MnXqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2NUmyNFgoRjJ{NEW5NlA5RC:jPh?=
human HepG2 cells NWm2NWdFTnWwY4Tpc44h[XO|YYm= NXL2UoZVOjRiaB?= MYLJcoNz\WG|ZTDpckBodHWlb4PlJINwdnO3bYD0bY9vKGmwIHnud5VtcW5vcnXzbZN1[W62IHj1cYFvKEincFeyJINmdGy|IHHmeIVzKDJ2IHjyd{whTUN3ME2wMlI4KM7:TT6= NIDRc4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUi1OlA1QCd-MkG4OVYxPDh:L3G+
Hs575T M2X4XmZ2dmO2aX;uJIF{e2G7 MoX4NlAhdU1? MmO3NlQhcHK| NUPPPWlzUW6qaXLpeIlwdiCxZjDtWG9TKHCqb4PwbI9zgWyjdHnvckBqdiC2cnnwcIUudmWpYYTpeoUhcHWvYX6gTJM2PzWWIHPlcIx{KGG2IEKwJI1OKGGodHXyJFI1KGi{czDifUBqdW23bn;icI91KGGwYXz5d4l{ NFjpPY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S5NFE1QCd-MkO0PVAyPDh:L3G+
Hs578T NUT0SIJISW62aXnueoF{cX[nIHHzd4F6 NITnS2YzOCCvTR?= NW\SeJJoOTdiaILz MknjRY51cWmwdnHzbZZmKGGldHn2bZR6KGGpYXnud5QhfHKrcHzlMY5m\2G2aY\lJIh2dWGwIFjzOVc5XCClZXzsd{BifCB{MDDtUUBi\nSncjCxO{BpenNiYomgcIlocHRibXnjdo9{[2:yaXOgZY5idHm|aYO= MmrlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2OUCxOFgoRjJ|NEmwNVQ5RC:jPh?=
Hs575T MWnGeY5kfGmxbjDhd5NigQ>? M4POfFIxKG2P NYTnWFVROjRiaILz MmTLRYN1cX[jdHnvckBw\iCDTWDLJIlvKHS{aYDs[U1v\WejdHn2[UBpfW2jbjDId|U4PVRiY3XscJMh[XRiMkCgcW0h[W[2ZYKgNlQhcHK|IHL5JIludXWwb3Lsc5Qh[W6jbInzbZM> NX3PcmJrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0PVAyPDhpPkKzOFkxOTR6PD;hQi=>
L6 Mmq5SpVv[3Srb36gZZN{[Xl? M4OyT|IhdU1? MlH1OEBpenN? M2nlfWlv[3KnYYPlJIlvKGeudXPvd4UhfXC2YXvlJIlvKHKjdDDMOkBk\WyuczDheEAzKG2PIITy[YF1\WRiZn;yJFQhcHK|IIDvd5QhOzBibXnud{BCVVCNIHnubIljcXSxcjDjc41xd3WwZDDDJJRz\WG2bXXueC=> NFLGXW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUGyPFE3Oyd-MkmxNlgyPjN:L3G+
HepG2 M4r1NWZ2dmO2aX;uJIF{e2G7 MkPqNUBuVQ>? MoXZNlQhcHK| NY\Bb3hGUW6mdXP0bY9vKG:oIHfseYNwe2ViY3;ud5VueHSrb36gbY4hcHWvYX6gTIVxTzJiY3XscJMh[XRiMTDtUUBqdmO3YnH0[YQh\m:{IEK0JIhzew>? NW\VR2dHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2OVE6QDRpPkK4OlUyQTh2PD;hQi=>
Assay
Methods Test Index PMID
Western blot p-AMPK / AMPK / p-mTOR / mTOR / p-S6K / S6K ; TTP / p-STAT3 / STAT3 / c-Myc ; pACC / ACC / pS6 / S6 ; pSTAT3 (Ser727) / STAT3 / Jak2 / Cdk5 / pNFκB / Bcl-2 / Bcl-XL / c-Myc 24505341 26956973 26172303 28114390
Immunofluorescence LKB1 ; PAR ; CD86 / CD206 ; beta-catenin / AMPK 29601127 21422199 30899369 30854043
Growth inhibition assay Cell viability 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 (from reference)

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
Formula

C4H11N5.HCl

CAS No. 1115-70-4
Storage 3 years -20°C powder
2 years -80°C in solvent
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
NCT04169243 Not yet recruiting Behavioral: New Nordic Diet|Other: Control Gestational Diabetes Mellitus Göteborg University|Swedish Council for Working Life and Social Research September 2022 Not Applicable
NCT04931017 Not yet recruiting Drug: Extended Release Metformin Hydrochloride Lung Carcinoma National Cancer Institute (NCI) April 20 2022 Phase 2
NCT05131828 Not yet recruiting Drug: Metformin and clemastine in combination|Drug: Placebo Multiple Sclerosis Cambridge University Hospitals NHS Foundation Trust|University of Cambridge February 2022 Phase 2
NCT05181449 Not yet recruiting Behavioral: Twin Precision Treatment Type 2 Diabetes The Cleveland Clinic|Twin Health January 3 2022 Not Applicable

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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