Metformin HCl

Name: Metformin HCl
Brand: Selleck Chemicals
SKU: S1950
Rating: 5 (15 reviews)

For research use only. Not for use in humans.

Catalog No.S1950

15 publications

Molecular Weight(MW): 165.62

Metformin HCl decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis).

Selleck's Metformin HCl has been cited by 15 publications

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

PubMed: 25490448 ( 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 )

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 )

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

PubMed: 29351847 ( 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 )

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 )

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	Activity Description	PMID
human HepG2 cells	MlfiSpVv[3Srb36gZZN{[Xl?		MWqyOEBp	NYryZlhmUW6lcnXhd4UhcW5iZ3z1Z49{\SClb37zeY1xfGmxbjDpckBqdnO3bHnuMZJme2m\|dHHueEBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjCyOEBpenNuIFXDOVA:OC5{NzFOwG0v	Mm\DNlE5PTZyNEi=
human MDA-MB-231 cells	M17HZWZ2dmO2aX;uJIF{e2G7	MUKxJJRwKDJyIH3N	NXrmT\|ZNOjRiaB?=	M1:3WWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ\|MTDj[YxteyCjdDCxJJRwKDJyIH3NJIFnfGW{IEK0JIhzeyCkeTDNWHQh[XO\|YYmu	NWnQXGlWOjJ2NUmyNFg>
human HepG2 cells	MYXGeY5kfGmxbjDhd5NigQ>?	MVqxJI1O	NVTO[XlyOjRiaB?=	MWXS[YR2[3Srb36gc4Yh\2y3Y3;z[UBkd26\|dX3weIlwdiCrbjDpcpN2dGmwLYLld4l{fGGwdDDoeY1idiCKZYDHNkBk\WyuczDheEAyKG2PIHHmeIVzKDJ2IHjyd{BjgSCpbIXjc5NmKG:6aXThd4UhdWW2aH;kJIlvKHC{ZYPlcoNmKG:oIEKyMlIhdU1ib3[g[4x2[2:\|ZR?=	NHr3e2QzOzB{NUK0OC=>
mouse 3T3L1 cells	NXTWfZBETnWwY4Tpc44h[XO\|YYm=	NW\5W29sOSCvTR?=		MVnJcoR2[3Srb36gc4YhSU2SSzDwbI9{eGixconsZZRqd25iaX6gcY92e2ViM2SzUFEh[2WubIOgZZQhOSCvTTDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN?	NYjTcGVZOjV{MU[zO\|k>
human HepG2 cells	NHfDS2hHfW6ldHnvckBie3OjeR?=	NIXmcY8yKG2P	MojsNlQhcA>?	MX;BZ5RqfmG2aX;uJI9nKEGPUFugbY4hcHWvYX6gTIVxTzJiY3XscJMh[XO\|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJIdtfWOxbnXv[4Vv\XOrczDheEAyKG2PIHHmeIVzKDJ2IHjyd{BjgSCnbor5cYF1cWNiY3;sc5JqdWW2cnnjJIF{e2G7	M1vidVI3PDdzMEmw

... 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
Storage	2 years -80°C in solvent
Synonyms	N/A
Smiles	Cl.CN(C)C(=N)NC(N)=N

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-10-14)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03416127	Not yet recruiting	Drug: Propolis\|Drug: Metformin\|Drug: Placebo	Diabetes Mellitus Type 2	University of Guadalajara	October 30 2019	Phase 2
NCT03710343	Not yet recruiting	Drug: Metformin\|Drug: Placebo Oral Tablet	Cerebral Palsy\|Spastic\|Spastic Cerebral Palsy\|Cerebral Palsy Spastic\|Cerebral Palsy Mixed	Holland Bloorview Kids Rehabilitation Hospital\|The Hospital for Sick Children	September 1 2019	Phase 2
NCT03994744	Recruiting	Drug: PD-1 inhibitor\|Drug: Metformin	Small-cell Lung Cancer\|Small Cell Lung Carcinoma\|Small Cell Lung Cancer Recurrent\|Small Cell Lung Cancer Extensive Stage	Hunan Cancer Hospital\|Xiangya Hospital of Central South University\|Innovent Biologics (Suzhou) Co. Ltd.	August 20 2019	Phase 2

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Metformin HCl