Metformin, 657-24-9

Cat.No.:IC-0128550

Product Information

Biological Activity

Metformin (1,1-Dimethylbiguanide) primarily mediate activation of AMPK, a serine/threonine protein kinase involved in regulating cellular energy metabolism, leading to a reduction in mTOR signaling and protein synthesis in cancer cells. Metformin activates AMPK by inhibiting complex I of the mitochondrial respiratory chain [1]. Metformin treatment reduced 4T1 cell viability with IC50: 16 mM, 24 h; 8 mM, 48 h; 4 mM, 72 h [2].
Metformin inhibited a variety of breast cancer cells growth regardless of oestrogen receptor (ER), PR, HER2 or p53 status [3]. Metformin induced unique responses in the triple-negative (ER, PR and HER2 negative) breast cancer cell line MDA-MB-231, leading to an S phase cell cycle arrest and then increase apoptosis [4]. Metformin may also be effective against ER-positive breast cancers by inhibiting aromatase expression in tumour stroma [5].
Orally administered metformin (at plasma levels (2.7-10.3 mM)) also reduced tobacco carcinogeninduced lung tumourigenesis (NNK) in mice (tumour burden reduced by 53%) [6]. Metformin treatment significantly delayed the appearance of mammary adenocarcinomas, reduced the size of tumours and prolonged the lifespan of MMTV-Her2/Neu mice [7].
Metformin is indicated for treatment of hyperglycemia in type 2 diabetes and improves glycemic control without inducing hypoglycemia or weight gain [8]. Metformin can cross though the blood-brain barrier and induces cell autophagy [9].

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species

Mouse

Rat

Rabbit

Guinea pig

Hamster

Dog

Weight (kg)

0.02

0.15

1.8

0.4

0.08

10

Body Surface Area (m2)

0.007

0.025

0.15

0.05

0.02

0.5

Km factor

3

6

12

8

5

20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by  (Animal B Km / Animal A Km)
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Order Information

Size

Price($£©

Price(€)

Price(£¤/CNY£©

Price(£¤/JYP£©

100mg

$60.00

€ 72.00

£¤600.00

£¤11,940.00

1g

$199.00

€ 238.80

£¤1,990.00

£¤39,601.00

5g

$299.00

€ 358.80

£¤2,990.00

£¤59,501.00

Free Delivery on orders over $350.00.

Chemical Information

Molecular Weight

129.16

Formula

C4H11N5

CAS Number

 657-24-9

Purity

0.9998

Solubility

DMSO: 100 mg/mL (774.23 mM); Water: 50 mg/mL (387.12 mM)

Storage

-20¡ãC, protect from light

Reference

[1]. Brunmair B, Staniek K, Gras F, Scharf N, Althaym A, Clara R, Roden M, Gnaiger E, Nohl H, Waldhausl W, et al. 2004 Thiazolidinediones, like metformin, inhibit respiratory complex I: a common mechanism contributing to their antidiabetic actions? Diabetes 53 1052-1059.

[2]. A. Farahi, M.R. Abedini, H. Javdani, L. Arzi, E. Chamani, R. Farhoudi, et al. Crocin and metformin suppress metastatic breast cancer progression via VEGF and MMP9 downregulations: in vitro and in vivo studies.Mol. Cell. Biochem. (2021), pp. 1-11

[3]. Zhuang?Y, Miskimins?WK.?Cell cycle arrest in Metformin treated breast cancer cells involves activation of AMPK, downregulation of cyclin D1, and requires p27Kip1 or p21Cip1. J Mol Signal?2008;3:18.

[4]. Liu B, Fan Z, Edgerton SM, Deng XS, Alimova IN, Lind SE & Thor AD. 2009. Metformin induces unique biological and molecular responses in triple negative breast cancer cells. Cell Cycle 8 2031-2040.

[5]. Deng XS, Wang S, Deng A, Liu B, Edgerton SM, Lind SE, Wahdan-Alaswad R & Thor AD 2012 Metformin targets Stat3 to inhibit cell growth and induce apoptosis in triple-negative breast cancers. Cell Cycle 11 367-376.

[6]. Memmott RM, Mercado JR, Maier CR, Kawabata S, Fox SD & Dennis PA 2010 Metformin prevents tobacco carcinogen-induced lung tumorigenesis. Cancer Prevention Research 3 1066-1076.

[7]. Anisimov?VN, Berstein?LM, Egormin?PA, Piskunova?TS, Popovich?IG, Zabezhinski?MA, Kovalenko?IG, Poroshina?TE, Semenchenko?AV, Provinciali?M, Re?F, Franceschi?C: Effect of metformin on life span and on the development of spontaneous mammary tumors in HER-2/neu transgenic mice. Exp Gerontol?2005;?40: 685-693

[8]. Flory, J. & Lipska, K. Metformin in 2019. JAMA321, 1926-1927 (2019).

[9]. 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.

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