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Submit ReviewMetformin hydrochloride
Description: Activator of LKB1/AMPK; antidiabetic agent
Chemical Name: N,N-Dimethylimidodicarbonimidic diamide hydrochloride
Biological Activity for Metformin hydrochloride
Metformin hydrochloride is an antidiabetic agent; lowers plasma glucose levels and improves insulin sensitivity. Inhibits hepatic gluconeogenesis via activation of the LKB1/AMPK pathway. Displays antiproliferative effects in cancer cell lines via inhibition of mitochondrial complex I (MRC-1). Activates the aPKC-CBP pathway in neural precursors to promote neurogenesis. Activates autophagy. Identified by chemoinformatics as targeting human host proteins that interact with SARS-CoV-2. Metformin hydrochloride prevents brain atrophy, and slows the pace of aging across diverse tissues in animal studies.
Compound Libraries for Metformin hydrochloride
Metformin hydrochloride is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Epigenetics Library, Tocriscreen FDA-Approved Drugs and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.
Technical Data for Metformin hydrochloride
| M. Wt | 165.62 |
| Formula | C4H11N5.HCl |
| Storage | Store at RT |
| CAS Number | 1115-70-4 |
| PubChem ID | 14219 |
| InChI Key | OETHQSJEHLVLGH-UHFFFAOYSA-N |
| Smiles | NC(NC(N(C)C)=N)=N.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Metformin hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 16.56 | 100 | |
| DMSO | 3.31 | 20 with gentle warming |
Preparing Stock Solutions for Metformin hydrochloride
The following data is based on the product molecular weight 165.62. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 6.04 mL | 30.19 mL | 60.38 mL |
| 5 mM | 1.21 mL | 6.04 mL | 12.08 mL |
| 10 mM | 0.6 mL | 3.02 mL | 6.04 mL |
| 50 mM | 0.12 mL | 0.6 mL | 1.21 mL |
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Product Datasheets for Metformin hydrochloride
References for Metformin hydrochloride
References are publications that support the biological activity of the product.
Shaw et al (2005) The kinase LKB1 mediates glucose homeostasis in liver and therapeutic effects of MetF.. Science 310 1642 PMID: 16308421
Towler and Hardie (2007) AMP-activated protein kinase in metabolic control and Ins signalling. Circ.Res. 100 328 PMID: 17307971
Hirsch et al (2013) MetF. inhibits the inflammatory response associated with cellular transformation and cancer stem cell growth. Proc.Natl.Acad.Sci.USA 110 972 PMID: 23277563
Wang et al (2012) MetF. activates an atypical PKC-CBP pathway to promote neurogenesis and enhance spatial memory formation. Cell Stem Cell 11 23 PMID: 22770240
Galluzzi et al (2017) Pharmacological modulation of autophagy: therapeutic potential and persisting obstacles. Nat.Rev.Drug.Discov. PMID: 28529316
Wheaton et al (2014) MetfF inhibits mitochondrial complex I of cancer cells to reduce tumorigenesis. Elife 3 e02242 PMID: 24843020
Gordon et al (2020) A SARS-CoV-2-human protein-protein interaction map reveals drug targets and potential drug-repurposing. Nature 583 PMID: 32353859
Yang et al (2024) Metformin decelerates aging clock in male monkeys. Cell 187 1 PMID: 39270656
If you know of a relevant reference for Metformin hydrochloride, please let us know.
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Keywords: Metformin hydrochloride, Metformin hydrochloride supplier, activators, LKB1/AMPK, antidiabetic, agent, AMP-Activated, Protein, Kinases, Enzyme, Substrates, mitochondrial, complex, I, MRC1, COVID-19, SARS-CoV-2, severe, acute, respiratory, syndrome, /, Activators, AMPK, Neural, Stem, Cells, Autophagy, Oxidative, Phosphorylation, Coronavirus, 2864, Tocris Bioscience
17 Citations for Metformin hydrochloride
Citations are publications that use Tocris products. Selected citations for Metformin hydrochloride include:
Bowling et al (2019) Altered steady state and activity-dependent de novo protein expression in fragile X syndrome. Nat Commun 10 1710 PMID: 30979884
Li et al (2016) Vitamin C alleviates aging defects in a stem cell model for Werner syndrome. Protein Cell 7 478 PMID: 27271327
Edris et al (2012) Comparative gene expression profiling of benign and malignant lesions reveals candidate therapeutic compounds for leiomyosarcoma. Sarcoma 2012 805614 PMID: 22919280
Valente et al (2014) OxLDL induces endothelial dysfunction and death via TRAF3IP2: inhibition by HDL3 and AMPK activators. Free Radic Biol Med 70 117 PMID: 24561578
Lin et al (2015) Development of telmis. in the therapy of spinal cord injury: pre-clinical study in rats. Nat Commun 9 4709 PMID: 26316709
Naka et al (2015) Dipeptide species regulate p38MAPK-Smad3 signalling to maintain chronic myelogenous leukaemia stem cells. BMC Cancer 6 8039 PMID: 26289811
Abdou et al (2014) A cell-autonomous molecular cascade initiated by AMP-activated protein kinase represses steroidogenesis. Mol Cell Biol 34 4257 PMID: 25225331
Yang et al (2024) Metformin decelerates aging clock in male monkeys. Cell 187 1 PMID: 39270656
Marinangeli et al (2018) AMP-Activated Protein Kinase Is Essential for the Maintenance of Energy Levels during Synaptic Activation. iScience 9 1 PMID: 30368077
Xintaropoulou et al (2018) Expression of glycolytic enzymes in ovarian cancers and evaluation of the glycolytic pathway as a strategy for ovarian cancer treatment. BMC Cancer 18 636 PMID: 29866066
Soliman et al (2017) Effects of MET and a Mammalian Target of Rapamycin (mTOR) ATP-Competitive Inhibitor on Targeted Metabolomics in Pancreatic Cancer Cell Line. Metabolomics (Los Angel) 6 PMID: 28217402
Yan et al (2015) Suppression of experimental arthritis through AMP-activated protein kinase activation and autophagy modulation. J Rheum Dis Treat 1 5 PMID: 26120598
Mo et al (2015) Cellular energy stress induces AMPK-mediated regulation of YAP and the Hippo pathway. Nat Cell Biol 17 500 PMID: 25751140
Yung et al (2013) Activation of AMPK inhibits cervical cancer cell growth through AKT/FOXO3a/FOXM1 signaling cascade. PLoS One 13 327 PMID: 23819460
Westergard et al (2019) Repeat-associated non-AUG translation in C9orf72-ALS/FTD is driven by neuronal excitation and stress. EMBO Mol Med 11 PMID: 30617154
Massey (2017) Modification of tumour cell metabolism modulates sensitivity to Chk1 inhibitor-induced DNA damage. Sci Rep 7 40778 PMID: 28106079
Xintaropoulou et al (2015) A comparative analysis of inhibitors of the glycolysis pathway in breast and ovarian cancer cell line models. Oncotarget 6 25677 PMID: 26259240
Do you know of a great paper that uses Metformin hydrochloride from Tocris? Please let us know.
Reviews for Metformin hydrochloride
Average Rating: 4 (Based on 2 Reviews.)
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Metformin treatment.
By
Anonymous on 03/21/2020
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: HPAF
1 mM add to media for 24 hours
AMPK activation.
By
Anonymous on 01/30/2018
Assay Type: Ex Vivo
Species: Mouse
Cell Line/Tissue: Brain slice
Used in brain slices to activate AMPK, but no effect on cell dynamic was found. No positive control was used though, so unsure if lack of effect is due to drug...
Pathways for Metformin hydrochloride
