Home Metabolism Carbohydrate Metabolism chemical - Autophagy activator - AMPK activator - Mitophagy activator - p38 MAPK activator - JNK activator Metformin Hydrochloride

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Metformin Hydrochloride Antihyperglycemic agent

Cat.No.S1950

Metformin Hydrochloride (1,1-Dimethylbiguanide Hydrochloride) is a highly effective Antihyperglycemic Agent, which primarily decreases hyperglycemia in hepatocytes by suppressing hepatic gluconeogenesis (glucose production by the liver). It also promotes mitophagy in mononuclear cells and induces apoptosis of lung cancer cells through activating the JNK/p38 MAPK pathway and GADD153.
Metformin Hydrochloride Carbohydrate Metabolism chemical Chemical Structure

Chemical Structure

Molecular Weight: 165.62

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability

Quality Control

Products Often Used Together with Metformin Hydrochloride

Melatonin

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

Cell Culture, Treatment & Working Concentration

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

Chemical Information, Storage & Stability

Molecular Weight 165.62 Formula

C4H11N5.HCl

 Storage (From the date of receipt)
CAS No. 1115-70-4 Download SDF Storage of Stock Solutions

Synonyms 1,1-Dimethylbiguanide HCl Smiles CN(C)C(=N)N=C(N)N.Cl

Solubility

In vitro
Batch:

Water : 33 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Mechanism of Action

Targets/IC50/Ki
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]
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]
References

Applications

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 S1950-WB1 24505341
Immunofluorescence LKB1 PAR CD86 / CD206 beta-catenin / AMPK S1950-IF1 29601127
Growth inhibition assay Cell viability S1950-viability1 26956973

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05910554 Not yet recruiting
Sarcoidosis Pulmonary
University of Maryland Baltimore
 May 1 2024 Phase 2
NCT06120881 Recruiting
Type 2 Diabetes
University of California San Francisco|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)
 April 1 2024 Early Phase 1
NCT06147050 Not yet recruiting
Long COVID
Purpose Life Sciences
 April 2024 Phase 3
NCT06296836 Not yet recruiting
Diabetes Mellitus Type 2
University of Illinois at Chicago|Emily Hanners|Dulal Bhaumik|Avisek Datta|Peggy Choye|Hailey Soni|Annesti Elmasri|Julie Jun|Colin Goodman
 April 1 2024 Phase 4

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