Metformin (hydrochloride) 盐酸二甲双胍
| MDL | MFCD00012582 |
| EC | EINECS 214-230-6 |
| 别名 | 1,1-二甲基双胍盐酸盐; ?二甲双胍盐酸盐; Metformin HCl |
| CAS | 1115-70-4 |
| 分子式 | C4H12ClN5 |
| 分子量 | 165.62 |
| 纯度 | HPLC≥98% |
| 单位 | 瓶 |
| 生物活性 | 二甲双胍主要是通过对线粒体呼吸链复合物1的轻度和短暂抑制降低肝脏葡萄糖的产生。[1-7] |
| In Vitro | 二甲双胍以浓度依赖性方式抑制ESC的增殖。 A-ESC的IC50为2.45mM，N-ESC的IC50为7.87mM。二甲双胍对分泌期A-ESC中AMPK信号激活的激活作用显著高于增殖期细胞[3]。二甲双胍（0-500μM）以剂量依赖性方式降低糖原合成，在培养的大鼠肝细胞中IC50值为196.5μM[4]。二甲双胍显示细胞活力和对PC-3细胞的细胞毒性作用，IC50为5 mM [5]。 |
| In Vivo | 单独使用二甲双胍（100 mg/kg，口服）和使用异丙肾上腺素基团的二甲双胍（25,50,100 mg/kg）通过组织病理学分析减轻肌细胞坏死[1]。二甲双胍（> 900mg/kg /天，口服）导致Crl：CD（SD）大鼠的濒死/死亡和临床毒性迹象[2]。 |
| SMILES | NC(NC(N(C)C)=N)=N.Cl |
| 靶点 | AMPK |
| 动物实验 | 将动物随机分成6组，每组6只大鼠。组1（对照）的大鼠接受皮下注射生理盐水（0.5mL）并在整个实验期间不进行治疗。组2中的大鼠口服给予二甲双胍（100mg/kg;每天两次）2天，并以24小时的间隔皮下注射盐水连续2天。组3（MI对照）的大鼠口服盐水（每天两次）2天，每天皮下注射异丙肾上腺素（100mg/kg）连续2天，间隔24小时。第4组至第6组的大鼠用25,50和100mg/kg的二甲双胍处理。将二甲双胍溶解在盐水中，并以12小时的间隔每天两次以0.25-0.5mL的体积强饲，在异丙肾上腺素注射之前立即开始。 |
| 细胞实验 | 将ESC以1×10 3个细胞/孔的浓度接种在96孔板中。附着后，用不同剂量的二甲双胍/化合物C处理细胞0分钟，15分钟，1小时和24小时。如前所述进行MTT测定。简言之，将MTT（5mg/mL）以10μL/孔的体积加入96孔板中，并将板孵育4小时。通过除去含有MTT的培养基终止MTT反应，并且每孔加入100μLDMSO并在室温下在振荡器上孵育10分钟以确保晶体充分溶解。吸光度值在595nm处测量。细胞增殖（对照的百分比）计算如下：吸光度（实验组）/吸光度（对照组）。如下计算细胞增殖抑制（对照的百分比）：100％细胞增殖（对照的百分比）。每个实验一式两份进行并重复六次以评估结果一致性。 |
| 数据来源文献 | [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. [2]. Quaile MP, et al. Toxicity and toxicokinetics of metformin in rats. Toxicol Appl Pharmacol. 2010 Mar 15;243(3):340-7. [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. [4]. Otto M, et al. Metformin inhibits glycogen synthesis and gluconeogenesis in cultured rat hepatocytes. Diabetes Obes Metab. 2003 May;5(3):189-94. [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. [6]. Nie L, et al. The Landscape of Histone Modifications in a High-Fat Diet-Induced Obese (DIO) Mouse Model. Mol Cell Proteomics. 2017 Jul;16(7):1324-1334. [7]. Zhang D, et al. Metformin ameliorates BSCB disruption by inhibiting neutrophil infiltration and MMP-9 expression but not direct TJ proteins expression regulation. J Cell Mol Med. 2017 Jul 12. |
| 规格 | 100mg 10mM*1mL (in Water) 500mg |
二甲双胍主要是通过对线粒体呼吸链复合物1的轻度和短暂抑制降低肝脏葡萄糖的产生。抑制肝脏中的线粒体呼吸链，导致 AMPK 活化，增强胰岛素敏感性，可用于2型糖尿病的研究。还可以透过血脑屏障，诱导自噬。
使用本产品的应用案例（仅供参考）
In Vitro
Cell （HepG2 cells，3.5 mg/L Metformin，24h）
HepG2 cells were seeded at a density of 5000 cells/well in 100 µL of DMEM medium in 96-well plates. HepG2 cell culture was maintained in a humidified atmosphere of 5% CO2 at 37℃. After incubated for 12 h, the cells were washed with PBS and the medium was replaced with DMEM high glucose medium supplemented with FBS (2%) and insulin (0.5×10-7 mol/L) and incubated for 36 h to build insulin-resistant HepG2 cells model. Subsequently, the cells were washed with serum-free DMEM high glucose medium and treated with different concentrations (0.1, 0.2, 0.4, and 0.8 mg/mL) of Up-3, Up-4, and Up-5. Medium and metformin (3.5 mg/L) were used as the normal and metformin group, respectively. After incubated for 24 h, the free supernatants of the cells were collected, and then the glucose concentration of supernatants was measured by a glucose test kit following the manufacturer’s protocol.
来源文献：Zhong QW, Zhou TS, Qiu WH, Wang YK, Xu QL, Ke SZ, Wang SJ, Jin WH, Chen JW, Zhang HW, Wei B, Wang H. Characterization and hypoglycemic effects of sulfated polysaccharides derived from brown seaweed Undaria pinnatifida. Food Chem. 2021 Mar 30;341(Pt 1):128148. doi: 10.1016/j.foodchem.2020.128148. Epub 2020 Sep 22. PMID: 33038776.
In Vivo
Mice（Eight-week-old Kunming mice (approximately 20–22 g, specific pathogen-free, SPF) ，200mg/kg，4h，口服）
Mice were orally treated with MET(200 mg/kg) for 4 h. Blood samples were subsequently taken from the angular vein.
来源文献：Zhang W, Gao J, Shen F, Ma X, Wang Z, Hou X, Hao E, Hou Y, Bai G. Cinnamaldehyde changes the dynamic balance of glucose metabolism by targeting ENO1. Life Sci. 2020 Oct 1;258:118151. doi: 10.1016/j.lfs.2020.118151. Epub 2020 Jul 26. PMID: 32726661.
