Metformin HCl

Catalog No.S1950

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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Cited by 12 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.

Purity & Quality Control

Choose Selective Carbohydrate Metabolism Inhibitors

Biological Activity

Description Metformin HCl decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis).
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 NXjGNIhVTnWwY4Tpc44h[XO|YYm= MYCyOEBp MkHzTY5kemWjc3WgbY4h\2y3Y3;z[UBkd26|dX3weIlwdiCrbjDpcpN2dGmwLYLld4l{fGGwdDDoeY1idiCKZYDHNkBk\WyuczDh[pRmeiB{NDDodpMtKEWFNUC9NE4zPyEQvF2u M2PzZlIyQDV4MES4
human MDA-MB-231 cells M3;IUWZ2dmO2aX;uJIF{e2G7 MnHKNUB1dyB{MDDtUS=> NUm3TIMzOjRiaB?= NYLoe2hmSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHH0JFEhfG9iMkCgcW0h[W[2ZYKgNlQhcHK|IHL5JG1VXCCjc4PhfU4> MmDyNlI1PTl{MEi=
human HepG2 cells NFrqc49HfW6ldHnvckBie3OjeR?= M1q2ZlEhdU1? MX6yOEBp M3\YOXJm\HWldHnvckBw\iCpbIXjc5NmKGOxboP1cZB1cW:wIHnuJIlve3WuaX6tdoV{cXO2YX70JIh2dWGwIFjldGczKGOnbHzzJIF1KDFibV2gZYZ1\XJiMkSgbJJ{KGK7IHfseYNwe2Vib4jp[IF{\SCvZYToc4QhcW5icILld4Vv[2Vib3[gNlIvOiCvTTDv[kBodHWlb4Pl MoT3NlMxOjV{NES=
mouse 3T3L1 cells NYjkOGQ3TnWwY4Tpc44h[XO|YYm= NGj2WFQyKG2P MVTJcoR2[3Srb36gc4YhSU2SSzDwbI9{eGixconsZZRqd25iaX6gcY92e2ViM2SzUFEh[2WubIOgZZQhOSCvTTDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? NGLyWXEzPTJzNkO3PS=>
human HepG2 cells NGPYSIJHfW6ldHnvckBie3OjeR?= NHuy[G8yKG2P MnPBNlQhcA>? Mn7ZRYN1cX[jdHnvckBw\iCDTWDLJIlvKGi3bXHuJGhmeEd{IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBodHWlb37lc4dmdmW|aYOgZZQhOSCvTTDh[pRmeiB{NDDodpMh[nliZX76fY1ifGmlIHPvcI9zcW2ndILpZ{Bie3OjeR?= Ml;UNlY1PzFyOUC=

... 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

* 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 powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03686657 Not yet recruiting Type 2 Diabetes|High Blood Pressure|Arthritis|Obesity ARKAY Therapeutics|Albany Medical College August 5 2019 Phase 1|Phase 2
NCT03499704 Not yet recruiting Diabetes Mellitus Type 2 Takeda August 31 2019 Phase 4
NCT03499704 Not yet recruiting Diabetes Mellitus Type 2 Takeda August 31 2019 Phase 4
NCT03686657 Not yet recruiting Type 2 Diabetes|High Blood Pressure|Arthritis|Obesity ARKAY Therapeutics|Albany Medical College August 5 2019 Phase 1|Phase 2
NCT03452267 Not yet recruiting Insulin Sensitivity Wayne State University June 2019 Phase 2|Phase 3
NCT03452267 Not yet recruiting Insulin Sensitivity Wayne State University June 2019 Phase 2|Phase 3

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID