Metformin HCl

Synonyms: 1,1-Dimethylbiguanide HCl

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

Metformin HCl Chemical Structure

CAS: 1115-70-4

Selleck's Metformin HCl has been cited by 86 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

Products often used together with Metformin HCl

Glyburide (Glibenclamide)


Metformin HCl and Glyburide are used in the treatment of type 2 diabetes mellitus.

Melatonin


Metformin HCl and Melatonin are effective in reduction of plasmatic levels of liver enzymes and decrease inflammatory response in rats.

Lemos AJJM, et al. Toxicol Appl Pharmacol. 2014 Oct 1;280(1):159-68.

Repaglinide


Metformin HCl and Repaglinide result in a reduction in glycated hemoglobin (HbA1c).

Kawamori R, et al. J Diabetes Investig. 2014 Feb 12;5(1):72-9.

Ertugliflozin


Metformin HCl and Ertugliflozin are used for the treatment of type 2 diabetes.

Frias JP, et al. Expert Rev Endocrinol Metab. 2019 Mar;14(2):75-83.

Etoposide


Metformin HCl and Etoposide increase mortality in B-CPAP and SW-1736 cells and reduce toxicity of these drugs in the normal cell lines.

Ghavami G, et al. Res Pharm Sci. 2023 Jan 19;18(2):185-201.

Metformin HCl Related Products

Choose Selective Carbohydrate Metabolism Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HepG2 cells Function assay 1 mM 24 h Activation of AMPK in human HepG2 cells assessed as reduction of gluconeogenesis at 1 mM after 24 hrs by enzymatic colorimetric assay 26471090
mouse 3T3L1 cells Function assay 1 mM Induction of AMPK phosphorylation in mouse 3T3L1 cells at 1 mM by Western blot analysis 25216379
human HepG2 cells Function assay 1 mM 24 h Reduction of glucose consumption in insulin-resistant human HepG2 cells at 1 mM after 24 hrs by glucose oxidase method in presence of 22.2 mM of glucose 23025244
human MDA-MB-231 cells Function assay 1 to 20 mM 24 h Antiproliferative activity against human MDA-MB-231 cells at 1 to 20 mM after 24 hrs by MTT assay. 22459208
human HepG2 cells Function assay 24 h Increase in glucose consumption in insulin-resistant human HepG2 cells after 24 hrs, EC50=0.27 μM. 21856048
Hs575T Function assay 20 mM 24 hrs Inhibition of mTOR phosphorylation in triple-negative human Hs575T cells at 20 mM after 24 hrs by immunoblot analysis 23490148
Hs578T Antiinvasive assay 20 mM 17 hrs Antiinvasive activity against triple-negative human Hs578T cells at 20 mM after 17 hrs by light microscopic analysis 23490148
Hs575T Function assay 20 mM 24 hrs Activation of AMPK in triple-negative human Hs575T cells at 20 mM after 24 hrs by immunoblot analysis 23490148
L6 Function assay 2 mM 4 hrs Increase in glucose uptake in rat L6 cells at 2 mM treated for 4 hrs post 30 mins AMPK inhibitor compound C treatment 29128163
HepG2 Function assay 1 mM 24 hrs Induction of glucose consumption in human HepG2 cells at 1 mM incubated for 24 hrs 28651984
Click to View More Cell Line Experimental Data

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
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 Research Cell lines Rat primary hepatocytes
Concentrations 500 µM
Incubation Time 1 h
Method

Cells were treated with different concentrations of metformin.

Experimental Result Images Methods Biomarkers Images 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
Immunofluorescence LKB1 PAR CD86 / CD206 beta-catenin / AMPK 29601127
Growth inhibition assay Cell viability 26956973
In Vivo
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]

Animal Research Animal Models Male Sprague-Dawley rats
Dosages 100 mg/300 mg
Administration o.g.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06147050 Not yet recruiting
Long COVID
Trust for Vaccines and Immunization Pakistan
January 2024 Phase 3
NCT06120881 Not yet recruiting
Type 2 Diabetes
University of California San Francisco|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)
December 1 2023 Early Phase 1
NCT06160414 Not yet recruiting
Healthy
Alexion Pharmaceuticals Inc.
December 13 2023 Phase 1
NCT05847244 Recruiting
Diastolic Dysfunction|Obesity
Sara ElAdawy|Cairo University|October University for Modern Sciences and Arts
October 1 2023 Phase 2

Chemical Information & Solubility

Molecular Weight 165.62 Formula

C4H11N5.HCl

CAS No. 1115-70-4 SDF Download Metformin HCl SDF
Smiles CN(C)C(=N)N=C(N)N.Cl
Storage (From the date of receipt)

In vitro
Batch:

Water : 33 mg/mL

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Metformin HCl | Metformin HCl ic50 | Metformin HCl price | Metformin HCl cost | Metformin HCl solubility dmso | Metformin HCl purchase | Metformin HCl manufacturer | Metformin HCl research buy | Metformin HCl order | Metformin HCl mouse | Metformin HCl chemical structure | Metformin HCl mw | Metformin HCl molecular weight | Metformin HCl datasheet | Metformin HCl supplier | Metformin HCl in vitro | Metformin HCl cell line | Metformin HCl concentration | Metformin HCl nmr