Metformin (glycinate)  (Synonyms: 1,1-Dimethylbiguanide (glycinate))

Metformin (1,1-Dimethylbiguanide) glycinate inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin glycinate exerts central glucose-lowering effects by inhibiting Ras-related protein 1 (Rap1) in SF1 hypothalamic neurons. Metformin glycinate also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, Metformin glycinate regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo^{[1][2][3][4][5][6][7][8]}.

Metformin (1,1-Dimethylbiguanide) glycinate inhibits proliferation of ESCs in a concentration-dependent manner. The IC₅₀ is 2.45 mM for A-ESCs and 7.87 mM for N-ESCs. Metformin glycinate shows pronounced effects on activation of AMPK signaling in A-ESCs from secretory phase than in cells from proliferative phase^[3].
Metformin (0-500 μM) glycinate decreases glycogen synthesis in a dose-dependent manner with an IC₅₀ value of 196.5 μM in cultured rat hepatocytes^[4].
Metformin glycinate shows cell viability and cytotoxic effects on PC-3 cells with IC₅₀ of 5 mM^[5].
Metformin (1–50 mM; 0-120 h) glycinate significantly inhibites the proliferation of both 786-O and OS-RC-2 RCC cell lines in a dose- and time-dependent manner^[7].
Metformin (5 mM; 0-48 h) glycinate stimulates AMPK and inhibited the mTOR signaling pathway in 786-O cells^[7].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Metformin (1,1-Dimethylbiguanide; 100 mg/kg, p.o.) glycinate alone, and metformin (25, 50, 100 mg/kg) with isoproterenol groups attenuates myocyte necrosis through histopathological analysis^[1].
Metformin (> 900 mg/kg/day, p.o.) glycinate results in moribundity/mortality and clinical signs of toxicity in Crl:CD(SD) rats^[2].
Metformin (200 mg/kg; i.p.; once a day for 6 consecutive days before induction of ischemia and at the beginning of reperfusion) glycinate significantly reduces the serum alanine aminotransferase (ALT) level in rats with ischemia-reperfusion model^[6].
Metformin (250 mg/kg; i.p.; once daily for 22 days) glycinate significantly reduces the growth of 786-O cell xenograft tumors in nude mice^[7].
When dissolved in PBS, the solution is strongly alkaline. Before animal administration, the pH needs to be adjusted to neutral (pH=7) with hydrochloric acid (e.g., 1M HCl).

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

204.23

C₆H₁₆N₆O₂

121369-64-0

O=C(CN)O.N=C(NC(N(C)C)=N)N

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Soraya H, et al. Acute treatment with metformin improves cardiac function following isoproterenol induced myocardial infarction in rats. Pharmacol Rep. 2012;64(6):1476-84.  [Content Brief]

  [2]. Quaile MP, et al. Toxicity and toxicokinetics of metformin in rats. Toxicol Appl Pharmacol. 2010 Mar 15;243(3):340-7.  [Content Brief]

  [3]. Xue J, et al. Metformin inhibits growth of eutopic stromal cells from adenomyotic endometrium via AMPK activation and subsequent inhibition of AKT phosphorylation: a possible role in the treatment of adenomyosis. Reproduction. 2013 Aug 21;146(4):397-406.  [Content Brief]

  [4]. Otto M, et al. Metformin inhibits glycogen synthesis and gluconeogenesis in cultured rat hepatocytes. Diabetes Obes Metab. 2003 May;5(3):189-94.  [Content Brief]

  [5]. Avci CB, et al. Therapeutic potential of an anti-diabetic drug, metformin: alteration of miRNA expression in prostate cancer cells. Asian Pac J Cancer Prev. 2013;14(2):765-8.  [Content Brief]

  [6]. Abdel-Zaher AO, et al. Novel mechanistic insights of the potential role of gasotransmitters and autophagy in the protective effect of metformin against hepatic ischemia/reperfusion injury in rats. Naunyn Schmiedebergs Arch Pharmacol. 2025 Feb 6.  [Content Brief]

  [7]. Liu J, et al. Metformin inhibits renal cell carcinoma in vitro and in vivo xenograft. Urol Oncol. 2013 Feb;31(2):264-70.  [Content Brief]

  [8]. Lin HY, et al. Low-dose metformin requires brain Rap1 for its antidiabetic action. Sci Adv. 2025 Aug;11(31):eadu3700.  [Content Brief]