Tirzepatide (LY3298176), 99% purity 多肽

0 条评论 | 添加你的评论
  • 序列:YXEGTFTSDYSIXLDKIAQKAFVQWLIAGGPSSGAPPPS (X2 and X13 are α-amino isobutyric acid (Aib), S39 is L-serinamide, and K20 is N6-{N-(hydrogen icosanedioyl)-γ-Glu-bis[iminobis(ethylenoxy)acetyl]}-Lysine)
  • 分子式:C225H348N48O68
  • 分子量:4813.45

相关文档

批次之间数据可能略有差异

产品详情

  • 产品名称
    Tirzepatide (LY3298176), 99% purity 多肽
  • 序列
    YXEGTFTSDYSIXLDKIAQKAFVQWLIAGGPSSGAPPPS (X2 and X13 are α-amino isobutyric acid (Aib), S39 is L-serinamide, and K20 is N6-{N-(hydrogen icosanedioyl)-γ-Glu-bis[iminobis(ethylenoxy)acetyl]}-Lysine)
  • 三字母序列
    Tyr-{Aib}-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-{Aib}-Leu-Asp-Lys-Ile-Ala-Gln-{N6-{N-(hydrogen icosanedioyl)-γ-Glu-bis[iminobis(ethylenoxy)acetyl]}-Lys}-Ala-Phe-Val-Gln-Trp-Leu-Ile-Ala-Gly-Gly-Pro-Ser- Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2
  • 长度 (aa)
    39
  • 多肽纯度 (HPLC)
    99.67
  • 分子式
    C225H348N48O68
  • 分子量
    4813.45
  • 来源
    固相合成
  • 其他信息
    The Net Peptide Content (NPC) of current batch (MTFA30421-0830) is 91.17%.

    Tirzepatide (LY3298176) is a dual GIP and GLP-1 receptor agonist under development for the treatment of type 2 diabetes mellitus (T2DM), obesity, and nonalcoholic steatohepatitis. Early phase trials in T2DM indicate that tirzepatide improves clinical outcomes beyond those achieved by a selective GLP-1 receptor agonist. Tirzepatide was discovered by engineering GLP-1 activity into the GIP sequence. It is an imbalanced dual agonist in favor of GIPR over GLP-1R activity as the molecule shows equal affinity for the GIPR compared with native GIP but binds the GLP-1R with approximately 5-fold weaker affinity than native GLP-1. The imbalanced nature of tirzepatide may be critical to maximizing the efficacy of a dual agonist because dose escalation for GLP-1R activation can be limited by gastrointestinal effects such as nausea and vomiting, while GIPR engagement is not known to be associated with similar events. As a consequence, a pharmacological profile favoring potency at the GIPR offers an opportunity to fully engage this pathway while minimizing GLP-1–related tolerability issues. In addition to a potency ratio toward GIPR activity, tirzepatide contains a C20 unsaturated di-acid acyl chain to affect albumin binding, and the overall properties of the molecule enable once-weekly dosing. Beyond convenience, this pharmacokinetic feature may confer pharmacodynamic benefit, as high and sustained concentrations of selective GLP-1R agonists have enhanced clinical efficacy.

    Notes:

    • *Tirzepatide (LY3298176) is lyophilized in a package of 5mg/tube.
    • Store lyophilized Tirzepatide (LY3298176) in a refrigerator at -20°C to 4°C (-4°F to 39°F)
    • If needed, liquid Tirzepatide (LY3298176) can be stored unrefrigerated at temperatures not to exceed 30ºC (86ºF) for up to 3 weeks.
    • Do not freeze liquid Tirzepatide (LY3298176).
    • Store Tirzepatide (LY3298176) in the original tube and protect it from light.
    • This product is not sterile, please sterilize it by filtration before cell assays or animal experiments.
  • 储存指南
    一般情况下, Tirzepatide (LY3298176), 99% purity 多肽 粉末应该保存在-20甚至-70摄氏度. Tirzepatide (LY3298176), 99% purity 多肽 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
  • 参考文献
    • Willard FS, Douros JD, Gabe MB, Showalter AD, Wainscott DB, Suter TM, et al. Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist. JCI Insight. 2020;5(17)
    • Min T, Bain SC. The Role of Tirzepatide, Dual GIP and GLP-1 Receptor Agonist, in the Management of Type 2 Diabetes: The SURPASS Clinical Trials. Diabetes Ther. 2021;12(1):143-157
    • Willard FS, Douros JD, Gabe MB, Showalter AD, Wainscott DB, Suter TM, et al. Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist. JCI Insight. 2020;5(17)
  • 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

  • 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。

多肽合成服务: 纽普生物(NovoPro)提供常规多肽合成、糖修饰多肽合成、稳定同位素标记的多肽合成、磷酸化多肽合成、荧光标记多肽、多肽的BSA/KLH/OVA等载体蛋白的偶联等服务

声明:本公司出售产品只能用于科研目的,不得用于诊断或者治疗!