Metformin HCl 盐酸二甲双胍;Acarbose 阿卡波糖;Antidiabetic drug抗糖尿病药物;Streptozotocin (STZ) 链脲佐菌素;CAS:1115-70-4;
产品信息
产品名称 | 产品编号 | 规格 | |
Metformin Hydrochloride 盐酸二甲双胍 | MZ3403-1G | 1g | |
Metformin Hydrochloride 盐酸二甲双胍 | MZ3403-5G | 5g | |
Metformin Hydrochloride 盐酸二甲双胍 | MZ3403-25G | 25g |
产品描述
盐酸二甲双胍(Metformin Hydrochloride)是最有效和普遍使用的II型糖尿病治疗药物之一,能够降低肝细胞中高血糖症,主要通过抑制肝糖原的产生(肝脏糖异生作用)发挥作用。二甲双胍(500μM)激活肝细胞AMPK,导致乙酰辅酶A羧化酶(ACC)活性下降,诱导脂肪酸氧化,抑制脂肪生成酶表达。二甲双胍(2mM)激活肌肉AMPK,促进葡萄糖摄取。二甲双胍降低肝脏葡萄糖生成,增加肌肉细胞葡萄糖摄取[1]。二甲双胍需要肝脏中的LKB1降低血糖浓度。二甲双胍(250mg/kg,腹腔注射)以LKB1依赖的方式增加正常饮食小鼠的肝脏AMPK活性以及降低高脂饮食小鼠内的血糖水平超过50%。还能减低ob/ob小鼠40%的血糖[2]。饮食诱导肥胖症的小鼠注射二甲双胍(10mg/kg/天或50mg/kg/天),能够降低体重增加、肝脏脂滴含量,和血浆中总的胆固醇、LDL-胆固醇和甘油三酯水平[3]。二甲双胍(250mg/kg)能够减少HCT116 p53–人结肠癌小鼠移植瘤模型中的肿瘤生长,但对过表达重组酿酒酵母Ndi NADH脱氢酶的HCT116 p53–肿瘤没效应[4]。
产品特性
1) CAS NO:1115-70-4
2) 化学名:N,N-Dimethylimidodicarbonimidic diamide hydrochloride
3) 同义名:Metformin HCl; 1,1-Dimethylbiguanide hydrochloride;
4) 分子式:C4H12ClN5
5) 分子量:165.62
6) 纯度:>98%
7) 外观:白色结晶或结晶性粉末
8) 溶解性:溶于水(100mM)、DMSO(50mM)
9) 化学结构式:
保存与运输方法
保存:室温干燥保存,或置于-20℃长期干燥保存,至少2年有效。
运输:室温运输。
注意事项
1) 本品并非商业化的临床药物,仅用作科研用途,不得用作临床诊断或治疗,不得用于食品或药品,绝对禁止用在人身上。
2) 为了您的安全和健康,请穿实验服并戴一次性手套操作。
配制储存液
质量
溶剂体积 浓度 |
1mg | 5mg | 10mg |
1mM | 6.0379 mL | 30.1896 mL | 60.3792 mL |
5mM | 1.2076 mL | 6.0379 mL | 12.0758 mL |
10mM | 0.6038 mL | 3.0190 mL | 6.0379 mL |
50mM | 0.1208 mL | 0.6038 mL | 1.2076 mL |
使用方法【源自文献,仅作参考】
文献1,Wheaton WW et al. Metformin inhibits mitochondrial complex I of cancer cells to reduce tumorigenesis. Elife. 2014 May 13;3:e02242. PMID: 24843020
体内研究: 动物模型(Animal Model):Female J:Nu mice 给药剂量(Dosages):Female J:Nu mice were injected with 3 × 106Control-HCT 116 p53−/−or NDI1-HCT 116 p53−/−using a 27-gauge needle. 4 days post-injection mice were treated with water supplemented with metformin or water alone and fluid intake was monitored daily to ensure an effective dose of 1.25 mg/ml or 250 mg/kg of metformin. |
文献2,Abdulreda MH et al.Liraglutide Compromises Pancreatic β Cell Function in a Humanized Mouse Model. Cell Metab. 2016 Mar 8;23(3):541-6. PMID: 26876561
体内研究: 动物模型(Animal Model):C57BL/6 male mice fed a diet containing 60 kcal fat-derived calories 药物配制(Preparation):Metformin, dissolved in saline, was orally administered daily for 14 weeks. 注射剂量(Dosages):Metformin was administered at a dose of 10 mg/kg or 50 mg/kg. The control mice were administered with saline. |
参考文献
[1] Zhou G et al. Role of AMP-activated protein kinase in mechanism of metformin action. J Clin Invest. 2001 Oct;108(8):1167-74.
[2] Shaw RJ et al. The kinase LKB1 mediates glucose homeostasis in liver and therapeutic effects of metformin. Science. 2005 Dec 9;310(5754):1642-6.
[3] Kim EK et al. Metformin prevents fatty liver and improves balance of white/brown adipose in an obesity mouse model by inducing FGF21. Mediators Inflamm. 2016; 2016:5813030.
[4] Wheaton WW et al. Metformin inhibits mitochondrial complex I of cancer cells to reduce tumorigenesis. Elife. 2014 May 13;3:e02242.