Liraglutide 利拉鲁肽 Streptozotocin (STZ) 链脲佐菌素;CAS:204656-20-2

Liraglutide 利拉鲁肽; GLP-1受体激动剂;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:204656-20-2;

产品信息                                                                                                            

 产品名称  产品编号 C AS NO.  规格                 
 Liraglutide 利拉鲁肽  MZ7351-1MG       204656-20-2       1mg
 Liraglutide 利拉鲁肽           MZ7351-5MG  204656-20-2  5mg  
 Liraglutide 利拉鲁肽  MZ7351-10MG  204656-20-2  10mg  

产品描述

利拉鲁肽(Liraglutide)是一种长效的胰高血糖素样肽-1(GLP-1)受体激动剂,是GLP-1 (7-37)的合成衍生物含有一个棕榈酸基团[1]。表达人GLP-1受体的CHO细胞内利拉鲁肽能够提高cAMP累积(EC50=61 pM)。体外原代新生大鼠胰岛β-细胞利拉鲁肽(100-1000 nM)能够抑制细胞因子和游离脂肪酸诱导的凋亡,分别超过95%和50%,这一效应会被GLP-1受体拮抗剂exendin-3 (9-39)和PI3K抑制剂渥曼青霉素所阻断[2]。补充膳食诱导的大鼠肥胖模型中,利拉鲁肽(0.2mg/kg,皮下注射,一天两次)降低卡路里摄取,改变饮食偏好到更高的食物与糖果比例,逆转体重和脂肪增加,以及增高胰岛素敏感性[3]。含利拉鲁肽的配方可用作辅助药物来治疗II型糖尿病,以及用于超重或肥胖成人的慢性体重控制。

产品特性

1)  CAS NO:204656-20-2

2)  化学名:L-histidyl-L-alanyl-L-α-glutamylglycyl-L-threonyl-L-phenylalanyl-L-threonyl-L-seryl-L-α-aspartyl- L-valyl-L-seryl-L-seryl-L-tyrosyl-L-leucyl-L-α-glutamylglycyl-L-glutaminyl-L-alanyl-L-alanyl-N6-[N-(1-oxohexadecyl)-L-γ-glutamyl]-L-lysyl-L-α-glutamyl-L-phenylalanyl-L-isoleucyl-L-alanyl-L-tryptophyl-L-leucyl-L-valyl-L-arginylglycyl-L-arginyl-glycine

3)   序列:H-His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys(γ -Glu- palmitoyl)-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg- Gly-Arg-Gly-OH

4)   同义名:Victoza, Liraglutida, Liraglutidum, NN 2211, NN-2211

5)   分子式:C172H265N43O51

6)   分子量:3751.2

7)   纯度:≥98%

8)   外观:白色至类白色粉末

9)   溶解性:溶于稀氨水、溶于水(1mg/ml)

保存与运输方法

保存:-20℃避光干燥保存,至少2年有效。

运输:冰袋运输。

注意事项

1)   针对溶解性比较差的化合物,可通过37℃孵育以及超声的方式来促进其溶解。

2)   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。  

3)   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  0.2666 mL            1.3329 mL          2.6658 mL       
 5mM  0.0533 mL  0.2666 mL  0.5332 mL
 10mM  0.0267 mL  0.1333 mL  0.2666 mL

使用方法【源自文献,仅作参考】

文献1,Raun K et al. Liraglutide, a Long-Acting Glucagon-Like Peptide-1 Analog, Reduces Body Weight and Food Intake in Obese Candy-Fed Rats, Whereas a Dipeptidyl Peptidase-IV Inhibitor, Vildagliptin, Does Not. Diabetes. 2007 Jan;56(1):8-15. PMID: 17192459

体内研究:

动物模型(Animal Model):Sprague-Dawley female rats

给药剂量(Dosages):After the initial 12 weeks, the candy-fed (DIO) rats were further randomized into treatment groups for another 12 weeks: 1) liraglutide 0.2 mg/kg s.c. twice daily (n = 10), 2) vildagliptin 10 mg/kg twice daily orally (n = 10), 3) control vehicle twice daily subcutaneously (n = 7), 4) control vehicle twice daily orally (n = 7), and 5) DIO-Chow (candy excluded from diet, reverting to chow only) plus vehicle twice daily orally (n = 10).

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):Human islets transplanted into the anterior chamber of the eye of streptozotocin (STZ)-induced diabetic nude mice.

药物配制(Preparation):A 1000x stock solution was prepared by dissolving 18 mg in 1 ml of sterile normal saline solution (0.9% sodium chloride), divided in single-use aliquots, and stored at−20°C.

注射剂量(Dosages):Nonfasting glycemia before and ~35 days after human islet intraocular transplantation in diabetic nude mice treated with liraglutide (300 μg/kg/day s.c.) or saline (control). Daily liraglutide or saline treatments were started two days prior to transplantation (n = 14 mice/treatment).

参考文献

[1] Knudsen LB et al.Potent derivatives of glucagon-like peptide-1 with pharmacokinetic properties suitable for once daily administration. J Med Chem. 2000 May 4;43(9):1664-9.

[2] Bregenholt S et al. The long-acting glucagon-like peptide-1 analogue, liraglutide, inhibits beta-cell apoptosis in vitro. Biochem Biophys Res Commun. 2005 May 6;330(2):577-84.

[3] Raun K et al. Liraglutide, a Long-Acting Glucagon-Like Peptide-1 Analog, Reduces Body Weight and Food Intake in Obese Candy-Fed Rats, Whereas a Dipeptidyl Peptidase-IV Inhibitor, Vildagliptin, Does Not. Diabetes. 2007 Jan;56(1):8-15.