Home PI3K/Akt/mTOR AMPK activator - Mitophagy activator - Apoptosis related activator - JNK activator - p38 MAPK activator Metformin For research use only.

Metformin

Synonyms: 1,1-Dimethylbiguanide

Metformin (1,1-Dimethylbiguanide), a widely used drug for treatment of type 2 diabetes, activates AMP-activated protein kinase (AMPK) in hepatocytes. Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.

Metformin Chemical Structure

Metformin Chemical Structure

CAS No. 657-24-9

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Metformin Related Products

Signaling Pathway

AMPK Signaling Pathways

AMPK Signaling Pathway

Biological Activity

Description Metformin (1,1-Dimethylbiguanide), a widely used drug for treatment of type 2 diabetes, activates AMP-activated protein kinase (AMPK) in hepatocytes. Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.
Targets
AMPK [1] JNK [3] p38 MAPK [3]
In vitro
In vitro

Metformin upregulates BAX activation with facilitation of BIM, BAD and PUMA, downregulates Bcl-2 and Bcl-xl, also induces cytochrome c release from mitochondria into the cytoplasm, directly triggering caspase-9-mediated mitochondrial apoptosis.[4]
Cell Research Cell lines human hepatic stellate cells (HSCs) LX-2, rat HSCs T6, human hepatocyte L02 and rat hepatocyte BRL-3A
Concentrations 0-80 mM
Incubation Time 24 h
Method

The human hepatic stellate cells (HSCs) LX-2 is maintained in RPMI 1640 medium, rat HSCs T6, human hepatocyte L02 and rat hepatocyte BRL-3A were maintained in DMEM, which are both supplemented with 10% (v/v) FBS and 1% (v/v) penicillin/streptomycin sulfate at 37 ℃ in a humidified 5% CO2 incubator. Metformin and AICAR solutions are filtered through 0.22 μm millipore membrane filter units. CCK8 assay is used to detect the effects of different concentration of metformin and AICAR on the proliferation of hepatic stellate cells. T6 cells and LX-2 cells are treated with different concentration of metformin and AICAR for 24 h, and the expression of collagen and α - SMA protein are detected by Western blot. Cells are treated with 10 mM metformin and 0.5 mM AICAR for 24 h, and the expression of collagen and α - SMA protein are detected by Western blot. The mRNA levels of collagen I and α - SMA are detected by RT-qPCR.
In Vivo
In vivo

Metformin shows therapeutic effect of metformin in mouse model of liver fibrosis associated with nonalcoholic steatohepatitis (NASH) in which hepatic function, NASH lesions and fibrosis are improved.[4]
Animal Research Animal Models Male C57BL/6N mice
Dosages 10-200 mg/kg; 65 mg/kg
Administration i.p.
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

Chemical Information & Solubility

Molecular Weight 129.16 Formula

C4H11N5
CAS No. 657-24-9 SDF --
Smiles CN(C)C(=N)NC(N)=N
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 26 mg/mL ( (201.3 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 26 mg/mL

Ethanol : 26 mg/mL


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