Metformin Hydrochloride 盐酸二甲双胍 Streptozotocin (STZ) 链脲佐菌素 CAS:1115-70-4

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

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.