Metformin HCl

Name: Metformin HCl
Brand: Selleck Chemicals
SKU: S1950
Rating: 5 (36 reviews)

For research use only.

Catalog No.S1950

36 publications

CAS No. 1115-70-4

Metformin 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 36 publications

Cancer Cell, 2014, 26(6):840-50

PubMed: 25490448 ( click the link to review the publication )

Nat Commun, 2020, 11(1):3344

PubMed: 32620751 ( click the link to review the publication )

Theranostics, 2020, 10(24):10861-10873

PubMed: 33042258 ( click the link to review the publication )

Cell Death Dis, 2020, 8;11(6):427

PubMed: 32513919 ( click the link to review the publication )

Int J Oncol, 2020, 56(5):1140-1151

PubMed: 32319594 ( click the link to review the publication )

J Biomed Sci, 2020, 27(1):5

PubMed: 31928533 ( click the link to review the publication )

Biochem Biophys Res Commun, 2020, 522(3):704-708

PubMed: 31787232 ( click the link to review the publication )

Graefes Arch Clin Exp Ophthalmol, 2020, 258(3):557-564

PubMed: 31938854 ( click the link to review the publication )

Biol Pharm Bull, 2020, 43(1):129-137

PubMed: 31902918 ( click the link to review the publication )

Biomed Pharmacother, 2020, 129:110460

PubMed: 32768950 ( click the link to review the publication )

Oxid Med Cell Longev, 2020, 2020:8708236

PubMed: 32104542 ( click the link to review the publication )

Exp Ther Med, 2020, 20(2):1415-1422

PubMed: 32742376 ( click the link to review the publication )

Autophagy, 2020, 10.108

PubMed: 32013726 ( click the link to review the publication )

J Exp Clin Cancer Res, 2019, 38(1):50

PubMed: 30717766 ( click the link to review the publication )

Acta Pharmacol Sin, 2019, 40(10):1292-1302

PubMed: 31015738 ( click the link to review the publication )

Biomed Pharmacother, 2019, 109:2548-2560

PubMed: 30551515 ( click the link to review the publication )

Cancer Med, 2019, 10.1002/cam4.2723

PubMed: 31830378 ( click the link to review the publication )

Biochem Biophys Res Commun, 2019, 515(2):332-338

PubMed: 31153642 ( click the link to review the publication )

Mol Med Rep, 2019, 20(4):3633-3641

PubMed: 31485658 ( click the link to review the publication )

Med Sci Monit, 2019, 25:5389-5400

PubMed: 31325378 ( click the link to review the publication )

Pharm Biol, 2019, 57(1):98-104

PubMed: 30757944 ( click the link to review the publication )

Drug Deliv, 2019, 26(1):522-531

PubMed: 31090470 ( click the link to review the publication )

Mol Cell, 2018, 69(2):279-291

PubMed: 29351847 ( click the link to review the publication )

Cell Death Dis, 2018, 9(2):225

PubMed: 29445087 ( click the link to review the publication )
Mol Pharm, 2018, 15(8):3272-3284

PubMed: 29969038 ( click the link to review the publication )

Front Mol Neurosci, 2018, 11:98

PubMed: 29666569 ( click the link to review the publication )

J Mol Endocrinol, 2018, 60(4):285-297

PubMed: 29555819 ( click the link to review the publication )

BMC Cancer, 2017, 17(1):309

PubMed: 28464864 ( click the link to review the publication )

Sci Rep, 2017, 7(1):2169

PubMed: 28526884 ( click the link to review the publication )

Oncotarget, 2017, 8(37):62057-62068

PubMed: 28977926 ( click the link to review the publication )

Neurochem Res, 2016, 41(10):2719-2727

PubMed: 27350579 ( click the link to review the publication )

Sci Rep, 2016, 6:28611

PubMed: 27334428 ( click the link to review the publication )

Korean J Pediatr, 2016, 59(9):374-380

PubMed: 27721842 ( click the link to review the publication )

Oncotarget, 2015, 6(2):969-78

PubMed: 25504439 ( click the link to review the publication )

Luminescence, 2014, 29(1):65-73

PubMed: 23559485 ( click the link to review the publication )

Anal Chem Insights, 2012, 7:31-46

PubMed: 22904611 ( click the link to review the publication )

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). 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	Activity Description	PMID
human HepG2 cells	MlfjSpVv[3Srb36gZZN{[Xl?		MlXpNlQhcA>?	Mle1TY5kemWjc3WgbY4h\2y3Y3;z[UBkd26\|dX3weIlwdiCrbjDpcpN2dGmwLYLld4l{fGGwdDDoeY1idiCKZYDHNkBk\WyuczDh[pRmeiB{NDDodpMtKEWFNUC9NE4zPyEQvF2u	MkXYNlE5PTZyNEi=
human MDA-MB-231 cells	MYfGeY5kfGmxbjDhd5NigQ>?	Mn3iNUB1dyB{MDDtUS=>	NVLKOmhMOjRiaB?=	MXnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk0zOzFiY3XscJMh[XRiMTD0c{AzOCCvTTDh[pRmeiB{NDDodpMh[nliTWTUJIF{e2G7Lh?=	M4T4clIzPDV7MkC4
human HepG2 cells	M3;6UmZ2dmO2aX;uJIF{e2G7	MmjzNUBuVQ>?	Mm\LNlQhcA>?	M1fhWnJm\HWldHnvckBw\iCpbIXjc5NmKGOxboP1cZB1cW:wIHnuJIlve3WuaX6tdoV{cXO2YX70JIh2dWGwIFjldGczKGOnbHzzJIF1KDFibV2gZYZ1\XJiMkSgbJJ{KGK7IHfseYNwe2Vib4jp[IF{\SCvZYToc4QhcW5icILld4Vv[2Vib3[gNlIvOiCvTTDv[kBodHWlb4Pl	MVeyN\|AzPTJ2NB?=
mouse 3T3L1 cells	MVnGeY5kfGmxbjDhd5NigQ>?	M{TaeVEhdU1?		NEjZO5BKdmS3Y4Tpc44hd2ZiQV3QT{BxcG:\|cHjvdplt[XSrb36gbY4hdW:3c3WgN3Q{VDFiY3XscJMh[XRiMTDtUUBjgSCZZYP0[ZJvKGKub4SgZY5idHm\|aYO=	MUmyOVIyPjN5OR?=
human HepG2 cells	NGCxRXJHfW6ldHnvckBie3OjeR?=	NU\KSmxGOSCvTR?=	M1yydVI1KGh?	NGTQRpNC[3SrdnH0bY9vKG:oIFHNVGshcW5iaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKGeudXPvcoVw\2WwZYPpd{BifCBzIH3NJIFnfGW{IEK0JIhzeyCkeTDlcpp6dWG2aXOgZ49td3KrbXX0dolkKGG\|c3H5	M{fjV\|I3PDdzMEmw

... 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 PLoS One 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 Breast Cancer Res Treat 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 Oncotarget 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 PLoS One 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 Cancer Sci LKB1 location with or without 10 lmol/L metformin treatment in Capan-2 wtLKB1 cell line. Scale bar, 50 μm. PAR ; PubMed: 21422199 Mol Cancer Res 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 Am J Transl Res 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 Oncol Lett 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 Breast Cancer Res Treat 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

References

[4] Schmidt LJ, et al. Prostate, 2007, 67(10), 1111-1120.

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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 Download Metformin HCl SDF

Molecular Weight	165.62
Formula	C₄H₁₁N₅.HCl
CAS No.	1115-70-4
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	CN(C)C(=N)N=C(N)N.Cl

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-09-01)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02394652	Recruiting	Drug: Metformin\|Drug: Cisplatin\|Drug: FAZA	Uterine Cervical Neoplasms\|Squamous Cell Carcinoma\|Adenocarcinoma\|Carcinoma Adenosquamous	University Health Network Toronto	May 2022	Phase 2
NCT04477590	Not yet recruiting	Drug: EXERCISE TRAINING WITH OR WITHOUT MEDICATION	Metabolic Syndrome Protection Against\|Exercise Training\|Metformin\|Statins\|Angiotensin-Converting-Enzyme Inhibitor\|Fasting Intermittent\|Angiotensin Hypertension	University of Castilla-La Mancha\|Spanish Ministry of Economy and Comptetitiveness\|Servicio de Salud de Castilla-La Mancha (SESCAM)	September 7 2020	Not Applicable
NCT04267809	Not yet recruiting	Drug: Metformin Hydrochloride	Endoplasmic Reticulum Stress\|Viral Infection\|Yellow Fever	Singapore General Hospital\|Duke-NUS Graduate Medical School	August 2020	Phase 2
NCT04530383	Active not recruiting	Drug: Metformin Hydrochloride	Cystic Fibrosis-related Diabetes\|Cystic Fibrosis	University of Kansas Medical Center	August 22 2020	Phase 2

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Metformin HCl