目錄号 | MZ7351-1MG | 售價 | 1580.00元 | ||||||||||||||||||||||||||||||||||||||||||
規格 | 1mg | 運輸溫度 | 冰袋運輸 | ||||||||||||||||||||||||||||||||||||||||||
其他名稱 | Victoza, Liraglutida, Liraglutidum, NN 2211, NN-2211 | 保存溫度 | -20℃避光(guāng)幹燥保存 | ||||||||||||||||||||||||||||||||||||||||||
CAS号 | 204656-20-2 | 有效期 | 至少2年(nián)有效 | ||||||||||||||||||||||||||||||||||||||||||
應用 | 胰高(gāo)血糖素樣肽-1(GLP-1)受體激動劑 | 訂購數量 |
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産品簡介: Liraglutide 利拉魯肽
Liraglutide 利拉魯肽; GLP-1受體激動劑;Metformin HCl 鹽酸二甲雙胍;Acarbose 阿卡波糖;Antidiabetic drug抗糖尿病藥物(wù);Streptozotocin (STZ) 鏈脲佐菌素;CAS:204656-20-2;
産品信息
【溫馨提示】:見(jiàn)我司(MKBio)的小(xiǎo)分子化合物(wù)常見(jiàn)問題-懋康生(shēng)物(wù)。 【溫馨提示】:見(jiàn)我司(MKBio)整理的糖尿病模型建立-鏈脲佐菌素(STZ)。
産品描述 利拉魯肽(Liraglutide)是一(yī)種長(cháng)效的胰高(gāo)血糖素樣肽-1(GLP-1)受體激動劑,是GLP-1 (7-37)的合成衍生(shēng)物(wù)含有一(yī)個(gè)棕榈酸基團[1]。表達人GLP-1受體的CHO細胞内利拉魯肽能(néng)夠提高(gāo)cAMP累積(EC50=61 pM)。體外原代新生(shēng)大鼠胰島β-細胞利拉魯肽(100-1000 nM)能(néng)夠抑制細胞因子和遊離脂肪酸誘導的凋亡,分别超過95%和50%,這一(yī)效應會(huì)被GLP-1受體拮抗劑exendin-3 (9-39)和PI3K抑制劑渥曼青黴素所阻斷[2]。補充膳食誘導的大鼠肥胖模型中,利拉魯肽(0.2mg/kg,皮下(xià)注射,一(yī)天兩次)降低(dī)卡路(lù)裡(lǐ)攝取,改變飲食偏好到(dào)更高(gāo)的食物(wù)與糖果比例,逆轉體重和脂肪增加,以及增高(gāo)胰島素敏感性[3]。含利拉魯肽的配方可用作輔助藥物(wù)來治療II型糖尿病,以及用于超重或肥胖成人的慢(màn)性體重控制。
産品特性 1) CAS NO:204656-20-2 2) 化學名: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) 同義名:Victoza, Liraglutida, Liraglutidum, NN 2211, NN-2211 5) 分子式:C172H265N43O51 6) 分子量:3751.2 7) 純度:≥98% 8) 外觀:白(bái)色至類白(bái)色粉末 9) 溶解性:溶于稀氨水(shuǐ)、溶于水(shuǐ)(1mg/ml)
保存與運輸方法 保存:-20℃避光(guāng)幹燥保存,至少2年(nián)有效。 運輸:冰袋運輸。
注意事(shì)項 1) 針對溶解性比較差的化合物(wù),可通(tōng)過37℃孵育以及超聲的方式來促進其溶解。 2) 本品并非商業(yè)化的臨床藥物(wù),僅用作科研用途,不得用作臨床診斷或治療,不得用于食品或藥品,絕對禁止用在人身上(shàng)。 3) 為(wèi)了您的安全和健康,請穿實驗服并戴一(yī)次性手套操作。
配制儲存液
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文獻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 體内研究: 動物(wù)模型(Animal Model):Sprague-Dawley female rats 給藥劑量(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). |
文獻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 體内研究: 動物(wù)模型(Animal Model):Human islets transplanted into the anterior chamber of the eye of streptozotocin (STZ)-induced diabetic nude mice. 藥物(wù)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. 注射劑量(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). |
[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.
— —Written/Edited by V. Shallan【版權歸MKBio懋康所有】
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