产品详情
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产品名称
Retatrutide (LY3437943), 99.70% purity 多肽 (TFA已除)
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三字母序列
Tyr-{Aib}-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-{α-Me-Leu}-Leu-Asp-Lys-{diacid-C20-gamma-Glu-(AEEA)-Lys}-Ala-Gln-{Aib}-Ala-Phe-Ile-Glu-Tyr-Leu-Leu-Glu-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2 (Sodium salt)
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长度 (aa)
39
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多肽纯度 (HPLC, %)
99.7
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分子式
C221H342N46O68
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分子量(Da)
4731.33
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CAS No.
2381089-83-2
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PubChem CID
485663353
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来源
固相合成
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描述
Retatrutide is the first triple agonist peptide targeting the Glucagon, GLP-1, and GIP receptors (3G), the EC50 values are 5.79 nM, 0.0643 nM, and 0.775 nM respectively [1].
Among its predecessors, Liraglutide (Victoza, Saxenda), Exenatide (Byetta), Semaglutide (Ozempic, Rybelsus, Wegovy), Lixisenatide (Adlyxin), Dulaglutide ( Trulicity) are GLP-1 receptor agonists, Tirzepatide (Mounjaro) is a GLP-1/GIP dual receptor co-agonist. Survodutide is a Glucagon/GLP-1 dual receptor co-agonist.
Retatrutidere is administered subcutaneously, with a half-life of 6 days, and therefore can be injected weekly [2]. After 48 weeks, Retatrutide achieved 24.2% weight loss in obese or overweight patients and produced 17% weight loss in diabetic patients, making it arguably the most powerful pipeline today. In addition, Retatrutide also achieved up to 86% reduction in liver fat in patients with NASH (non-alcoholic steatohepatitis) [2].
A 48-week phase 2 obesity study demonstrated weight reductions of 22.8% and 24.2% with retatrutide 8 and 12 mg, respectively. The liver fat (LF) reduction at 24 weeks was -42.9% (1 mg), -57.0% (4 mg), -81.4% (8 mg), -82.4% (12 mg) and +0.3% (placebo)[3].
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储存指南
一般情况下, Retatrutide (LY3437943), 99.70% purity 多肽 (TFA已除) 粉末应该保存在-20甚至-70摄氏度. Retatrutide (LY3437943), 99.70% purity 多肽 (TFA已除) 溶解后应该-70摄氏度分装保存,避免反复冻融. 了解更多细节,请查阅手册:多肽溶解及保存指南
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参考文献
- 1. Coskun T, Urva S, Roell WC, Qu H, Loghin C, Moyers JS, O'Farrell LS, Briere DA, Sloop KW, Thomas MK, Pirro V, Wainscott DB, Willard FS, Abernathy M, Morford L, Du Y, Benson C, Gimeno RE, Haupt A, Milicevic Z. LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss: From discovery to clinical proof of concept. Cell Metab. 2022 Sep 6;34(9):1234-1247.e9.
- 2. Jastreboff AM, Kaplan LM, Frías JP, et al. Triple-Hormone-Receptor Agonist Retatrutide for Obesity - A Phase 2 Trial [published online ahead of print, 2023 Jun 26]. N Engl J Med. 2023;10.1056/NEJMoa2301972.
- 3. Sanyal, Arun J et al. “Triple hormone receptor agonist retatrutide for metabolic dysfunction-associated steatotic liver disease: a randomized phase 2a trial.” Nature medicine vol. 30,7 (2024): 2037-2048. doi:10.1038/s41591-024-03018-2
- 4. Ma, Jun et al. “Comparison of the effects of Liraglutide, Tirzepatide, and Retatrutide on diabetic kidney disease in db/db mice.” Endocrine, 10.1007/s12020-024-03998-8. 30 Aug. 2024, doi:10.1007/s12020-024-03998-8
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关于三氟乙酸盐
三氟乙酸(TFA)是一种强酸,常用于从固相树脂中裂解合成的多肽,也可用于提高多肽纯化步骤中的HPLC性能。默认情况下,定制的多肽是以冻干的TFA盐的形式交付的,其中TFA的含量可能高达10-45%。
定制多肽中的TFA可能会导致后续检测数据出现无法解释的差异。例如,nM浓度的TFA已被证明会干扰细胞实验,在某些情况下会抑制细胞增殖,而在其他情况下会增加细胞活力。
TFA去除服务推荐用于:
- 将用于细胞试验的多肽
- 将被用作原料药或制成品的多肽
- 含有大量碱性残基的亲水多肽
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关于多肽净含量
干品多肽的重量中不仅仅包含多肽,还包含有一些非肽的组份,如水、被吸收的溶剂、配位离子和盐等。肽的净含量是指肽在其中的重量百分比,这个百分比的数值范围很大,可能从50%到90%,取决于纯度、序列以及合成和纯化的方法,不要将肽的净含量和肽的纯度混为一谈,他们是两个完全不同的概念。纯度通常是通过HPLC测定的。纯度定义的是多肽样品中含正确序列的组分的百分比,而肽的净含量是指样品中肽类物质相对于总物质所占的百分比,肽的净含量通常是氨基酸组分分析或紫外分光法测定的,这个信息主要是在一些对肽的浓度很敏感的实验中,对计算肽的浓度是很重要的。
相关服务
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