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Metformin (1,1-Dimethylbiguanide) Antihyperglycemic Drug

Cat.No.S5958

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.
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Quality Control

Batch: Purity: 99.99%
99.99

Solubility

In vitro
Batch:

Water : 130 mg/mL

DMSO : 26 mg/mL (201.3 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 26 mg/mL

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

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Chemical Information, Storage & Stability

Molecular Weight 129.16 Formula

C4H11N5

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 657-24-9 -- Storage of Stock Solutions

Read more about storage stability stock solution CAS number

Mechanism of Action

Targets/IC50/Ki
AMPK
JNK
p38 MAPK
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.

In vivo

Metformin shows therapeutic effect of this compound in mouse model of liver fibrosis associated with nonalcoholic steatohepatitis (NASH) in which hepatic function, NASH lesions and fibrosis are improved.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/35344814/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-07-23)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07724132 RECRUITING
Alzheimer's Disease (AD); Mild Cognitive Impairment Due to Alzheimer's Disease; Alzheimer Disease Dementia
University College, London
2026-07-24 PHASE3
NCT07724132 RECRUITING
Alzheimer's Disease (AD); Mild Cognitive Impairment Due to Alzheimer's Disease; Alzheimer Disease Dementia
University College, London
2026-07-24 PHASE3
NCT01042379 RECRUITING
Breast Neoplasms; Breast Cancer; Breast Tumors; Angiosarcoma; TNBC - Triple-Negative Breast Cancer; HER2-positive Breast Cancer; HER2-negative Breast Cancer; Hormone Receptor Positive Tumor; Hormone Receptor Negative Tumor; Early-stage Breast Cancer; Locally Advanced Breast Cancer
QuantumLeap Healthcare Collaborative
2010-03-01 PHASE2
NCT01042379 RECRUITING
Breast Neoplasms; Breast Cancer; Breast Tumors; Angiosarcoma; TNBC - Triple-Negative Breast Cancer; HER2-positive Breast Cancer; HER2-negative Breast Cancer; Hormone Receptor Positive Tumor; Hormone Receptor Negative Tumor; Early-stage Breast Cancer; Locally Advanced Breast Cancer
QuantumLeap Healthcare Collaborative
2010-03-01 PHASE2
NCT06185179 RECRUITING
Muscle Atrophy or Weakness
University of Utah
2024-09-01 EARLY_PHASE1
NCT06185179 RECRUITING
Muscle Atrophy or Weakness
University of Utah
2024-09-01 EARLY_PHASE1

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