Metformin [657-24-9]

Metformin (1,1-Dimethylbiguanide) is an AMPK activator with blood-brain barrier permeability. Metformin may improve glycemic control by increasing insulin sensitivity and decreasing intestinal glucose uptake, and is commonly used in type 2 diabetes research.

Metformin, CAS 657-24-9

Description	Metformin (1,1-Dimethylbiguanide) is an AMPK activator with blood-brain barrier permeability. Metformin may improve glycemic control by increasing insulin sensitivity and decreasing intestinal glucose uptake, and is commonly used in type 2 diabetes research.
In vitro	METHODS: Ovarian cancer cells A2780 and SKOV3 were treated with Metformin (0.001-50 mM) for 24-48 h. Cell viability was assayed using the MTS RESULTS: Micromolar concentrations of Metformin did not statistically reduce the viability of the A2780 or SKOV3 cell lines. At 48 h, millimolar concentrations resulted in cell death. [1] METHODS: Human colorectal cancer cells HCT29 were treated with Metformin (0.6 mM) for 90 h. Cell motility was detected using the wound healing assay and chamber invasion assay. RESULTS: Metformin inhibited the migration and invasion of HCT29 cells, and Metformin decreased the motility of tumor cells. [2]
In vivo	METHODS: To model Metformin-induced diarrhea, Metformin (125-500 mg/kg) was administered orally to healthy and diabetic obese db/db C57BL/6J mice twice daily for thirteen days. RESULTS: Metformin at 1000 mg/kg/day significantly increased fecal water content. Although no diarrhea symptoms were observed in healthy C57BL/6J mice, the same dose of Metformin induced severe diarrhea in diabetic obese db/db mice. [3] METHODS: To investigate the protective effect of Metformin in radiation injury, Metformin (200 mg/kg once daily for three days) was administered orally to BALB/c mice, which were then exposed to 6-8 Gy of gamma radiation. RESULTS: When administered prior to exposure to radiation, Metformin prolonged the survival of mice exposed to 8 Gy-TBI and increased the survival of mice exposed to 6 Gy-TBI. Pretreatment with Metformin attenuated radiation damage. [4]

Synonyms	1,1-Dimethylbiguanide
Molecular Weight	129.16
Formula	C4H11N5
CAS No.	657-24-9

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 26 mg/mL (201.3 mM)

H2O: 26 mg/mL (201.3 mM)

References and Literature

1. Erices R, et al. Metformin, at concentrations corresponding to the treatment of diabetes, potentiates the cytotoxic effects of carboplatin in cultures of ovarian cancer cells. Reprod Sci. 2013 Dec;20(12):1433-46. 2. Mogavero A, et al. Metformin transiently inhibits colorectal cancer cell proliferation as a result of either AMPK activation or increased ROS production. Sci Rep. 2017 Nov 22;7(1):15992. 3. Takemori H, et al. Mouse model of metformin-induced diarrhea. BMJ Open Diabetes Res Care. 2020 Mar;8(1):e000898. 4. Da F, et al. Pretreatment with metformin protects mice from whole-body irradiation. J Radiat Res. 2021 Jul 10;62(4):618-625. 5. Jia Y, Cui R, Wang C, et al. Metformin protects against intestinal ischemia-reperfusion injury and cell pyroptosis via TXNIP-NLRP3-GSDMD pathway[J]. Redox Biology. 2020: 101534.

Citations

1. Ma W, Wu Q, Wang S, et al.A breakdown of metabolic reprogramming in microglia induced by CKLF1 exacerbates immune tolerance in ischemic stroke.Journal of Neuroinflammation.2023, 20(1): 1-23. 2. Zhang W, Li X, Jiang M, et al.SOCS3 deficiency-dependent autophagy repression promote the survival of early-stage myeloid-derived suppressor cells in breast cancer by activating the Wnt/mTOR pathway.Journal of Leukocyte Biology.2023: qiad020. 3. Fan P, Lu Y, Wei H, et al.Metformin attenuates sevoflurane-induced neurogenesis damage and cognitive impairment: involvement of the Nrf2/G6PD pathway.Metabolic Brain Disease.2023: 1-17. 4. Mlicka A, Mlicki P, Niewiadomski P, et al.Synergistic effect of metformin and doxorubicin on the metastatic potential of T24 cells.Acta Histochemica.2023, 125(1): 151975. 5. Jia Y, Cui R, Wang C, et al. Metformin protects against intestinal ischemia-reperfusion injury and cell pyroptosis via TXNIP-NLRP3-GSDMD pathway. Redox Biology. 2020: 101534. 6. Zhan Z T, Liu L, Cheng M Z, et al. The Effects of 6 Common Antidiabetic Drugs on Anti-PD1 Immune Checkpoint Inhibitor in Tumor Treatment. Journal of Immunology Research. 2022 7. Chen H, Sa G, He S, et al. In vitro and in vivo synergistic anti-tumor effect of LIN28 inhibitor and metformin in oral squamous cell carcinoma. European Journal of Pharmacology. 2021 Jan 15;891:173757. doi: 10.1016 8. Lan H, Dong Z W, Zhang M Y, et al.Sinapic acid modulates oxidative stress and metabolic disturbances to attenuate ovarian fibrosis in letrozole‐induced polycystic ovary syndrome SD rats.Food Science & Nutrition.2024