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Chemical Structure| 1115-70-4 Chemical Structure| 1115-70-4

Structure of Metformin HCl
CAS No.: 1115-70-4

Chemical Structure| 1115-70-4

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Metformin hydrochloride (1,1-Dimethylbiguanide hydrochloride) inhibits the mitochondrial respiratory chain in the liver, activating AMPK and enhancing insulin sensitivity, which is useful in type 2 diabetes research. It also triggers autophagy.

Synonyms: 1,1-Dimethylbiguanide hydrochloride; Metformin (hydrochloride); Metformin HCl

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Product Details of Metformin HCl

CAS No. :1115-70-4
Formula : C4H12ClN5
M.W : 165.62
SMILES Code : N=C(NC(N)=N)N(C)C.[H]Cl
Synonyms :
1,1-Dimethylbiguanide hydrochloride; Metformin (hydrochloride); Metformin HCl
MDL No. :MFCD00012582

Safety of Metformin HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Metformin HCl

epigenetics
PI3K-AKT

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Huh-7 cells 1 mM 8 h To evaluate the effect of Metformin on AMPK activation, results showed that Metformin treatment increased ACC phosphorylation, indicating AMPK activation. Sci Adv. 2016 Jul 27;2(7):e1600031.
MOLM14 cells 10 mM 24 h To evaluate the effect of Metformin on lipid metabolism in AML cells, results showed that Metformin treatment led to lipid droplet accumulation Nat Commun. 2020 Aug 13;11(1):4056.
U937 cells 10 mM 24 h To evaluate the effect of Metformin on lipid metabolism in AML cells, results showed that Metformin treatment led to lipid droplet accumulation Nat Commun. 2020 Aug 13;11(1):4056.
BT-474 cells 0.5 mmol/L 6 days To investigate the inhibitory effect of Metformin on HER2+ breast cancer cell proliferation, results showed that Metformin significantly inhibited cell proliferation Cancer Commun (Lond). 2021 May;41(5):414-431.
MDA-MB-361 cells 0.5 mmol/L 6 days To investigate the inhibitory effect of Metformin on HER2+ breast cancer cell proliferation, results showed that Metformin significantly inhibited cell proliferation Cancer Commun (Lond). 2021 May;41(5):414-431.
FAO rat hepatoma cells 200 μM 24 h Metformin reduced basal and activated glucose production by 46% and 40%, respectively. Diabetes. 2012 Aug;61(8):2146-54.
C4-2 cells 5 mM 48 h To investigate whether metformin can enhance the anti-tumor effect of enzalutamide on prostate cancer cells. The results showed that metformin or enzalutamide alone inhibited cell growth, but the combination of both had a more significant effect. Cell Death Dis. 2017 Aug 24;8(8):e3007.
CWR22Rv1 cells 5 mM 48 h To investigate whether metformin can enhance the anti-tumor effect of enzalutamide on prostate cancer cells. The results showed that metformin or enzalutamide alone inhibited cell growth, but the combination of both had a more significant effect. Cell Death Dis. 2017 Aug 24;8(8):e3007.
LNCaP cells 5 mM 48 h To investigate whether metformin can enhance the anti-tumor effect of enzalutamide on prostate cancer cells. The results showed that metformin or enzalutamide alone inhibited cell growth, but the combination of both had a more significant effect. Cell Death Dis. 2017 Aug 24;8(8):e3007.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice U2932 and SuDHL8 tumor models Intravenous injection 50 mg/kg Single dose, lasted for 30 min Evaluate the inhibitory effect of AMD3465 on CXCR4 expression, results showed metformin treatment significantly reduced the urinary excretion of [18F]MCFB Mol Pharm. 2019 May 6;16(5):2106-2117.
NSG mice AML MOLM14 cell engraftment model Oral 1.5 mg/kg Once daily for 17 days To evaluate the effect of IACS-010759 on AML cell proliferation and tumor growth, results showed that IACS-010759 significantly reduced tumor cell burden and increased overall survival in mice Nat Commun. 2020 Aug 13;11(1):4056.
Mice MMTV-ErbB2/Leprdb/db mouse model Oral 0.5 g/kg Once daily for 2 weeks To investigate the inhibitory effect of Metformin on tumor growth in a diabetic HER2+ breast cancer mouse model, results showed that Metformin significantly inhibited tumor growth and improved insulin tolerance Cancer Commun (Lond). 2021 May;41(5):414-431.
C57BL/6 mice High-fat diet-induced obese mice Oral 200 mg/kg Three times a week for eight weeks As a positive control, Metformin significantly reduced, weight gain, and white adipocyte size, and improved obesity-induced serum levels of glucose, free fatty acid, total TG, and total cholesterol in high-fat diet-induced obese mice. Nutrients. 2020 Apr 27;12(5):1242
Mice High-fat diet-streptozotocin-induced diabetic model Oral 450 mg/kg Once daily for 8 weeks To assess the effects of metformin on cardiovascular function in diabetic mice after myocardial infarction, showing that metformin treatment reduced mortality post-MI. Diabetes. 2010 Apr;59(4):1063-73
Db/db mice Diabetic model Oral gavage 300 mg/kg Once daily for 2-4 weeks Metformin reduced fasting blood glucose levels in db/db mice, and the effect was more pronounced when combined with MTZ. Diabetes. 2012 Aug;61(8):2146-54.
Nude mice H460 cell xenograft model Oral 350 mg/kg Once daily for 14 days Metformin significantly inhibited tumor growth and induced apoptosis and enhanced TRAIL expression in vivo. Mol Ther Oncolytics. 2021 Apr 29;21:303-314
Nude mice CWR22Rv1 xenograft model Esophageal gavaging 300 mg/kg Once daily for 3 weeks To test whether metformin can reverse the resistance of CWR22Rv1 cells to enzalutamide. The results showed that metformin alone reduced tumor size and weight, and the combination of metformin and enzalutamide had a more significant effect. Cell Death Dis. 2017 Aug 24;8(8):e3007.

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00187798 Other Conditions That May Be A... More >> Focus of Clinical Attention Less << COMPLETED 2025-07-07 University of California San F... More >>rancsico, San Francisco, California, 94143, United States Less <<
NCT00944346 Healthy PHASE1 COMPLETED - Gateway Medical Research, Inc.... More >>, St, Charles, Missouri, United States Less <<
NCT00944177 Healthy PHASE1 COMPLETED - Gateway Medical Research, Inc.... More >>, St, Charles, Missouri, United States Less <<
NCT04545736 ABCA4 Retinopathy|Stargardt Di... More >>sease|Retinal Dystrophy|Retinal Degeneration Less << PHASE1|PHASE2 RECRUITING 2028-09-30 National Institutes of Health ... More >>Clinical Center, Bethesda, Maryland, 20892, United States|University of Michigan, Ann Arbor, Michigan, 48109-0624, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

6.04mL

1.21mL

0.60mL

30.19mL

6.04mL

3.02mL

60.38mL

12.08mL

6.04mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

[1]Dos Santos CC, Gopal B, Verma S. Metformin: An Old Dog with a New Trick?. Cell Metab. 2018;28(3):334-336。

[2]Qin N, Li CB, et al. Synthesis and biological activity of novel tiliroside derivants. Eur J Med Chem. 2011;46(10):5189-95.

[3]Polianskyte-Prause Z, Tolvanen TA, et al. Metformin increases glucose uptake and acts renoprotectively by reducing SHIP2 activity. FASEB J. 2019;33(2):2858-2869.

[4]Takiyama Y, Harumi T, et al. Tubular injury in a rat model of type 2 diabetes is prevented by metformin: a possible role of HIF-1α expression and oxygen metabolism. Diabetes. 2011;60(3):981-92.

[5]Luo T, Nocon A, et al. AMPK Activation by Metformin Suppresses Abnormal Extracellular Matrix Remodeling in Adipose Tissue and Ameliorates Insulin Resistance in Obesity. Diabetes. 2016;65(8):2295-310.

[6]Sesen J, Dahan P, et al. Metformin inhibits growth of human glioblastoma cells and enhances therapeutic response. PLoS One. 2015;10(4):e0123721.

[7]Jenkins AJ, Welsh P, Petrie JR. Metformin, lipids and atherosclerosis prevention. Curr Opin Lipidol. 2018;29(4):346-353.

[8]Rangarajan S, Bone NB, et al. Metformin reverses established lung fibrosis in a bleomycin model. Nat Med. 2018;24(8):1121-1127.

[9]D'Amato G, Caringella AM, et al. Mild ovarian stimulation with letrozole plus fixed dose human menopausal gonadotropin prior to IVF/ICSI for infertile non-obese women with polycystic ovarian syndrome being pre-treated with metformin: a pilot study. Reprod Biol Endocrinol. 2018;16(1):89.

[10]Yan J, Yao B, et al. Liraglutide, Sitagliptin, and Insulin Glargine Added to Metformin: The Effect on Body Weight and Intrahepatic Lipid in Patients With Type 2 Diabetes Mellitus and Nonalcoholic Fatty Liver Disease. Hepatology. 2018.

[11]Rotermund C, Machetanz G, Fitzgerald JC. The Therapeutic Potential of Metformin in Neurodegenerative Diseases. Front Endocrinol (Lausanne). 2018.

 

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