[Glu2]TRH 多肽

Pyr-EP-NH2

Pyr-Glu-Pro-NH2

2

95.14

C₁₅H₂₂N₄O₆

354.36

85541-78-2

122148

固相合成

[Glu2]TRH is an endogenous peptide with the amino acid sequence pGlu-Glu-Pro-NH2. It is structurally related to thyrotropin-releasing hormone (TRH, pGlu-His-Pro-NH2). [Glu2]TRH is not metabolized by thyroliberinase, an enzyme that rapidly inactivates TRH, and is stable in rat serum for at least 4 hours, being cleared only by the kidneys. [Glu2]TRH does not bind with an appreciable affinity to the two known TRH-receptor isoforms (TRHR1 and TRHR2). [Glu2]TRH possesses intrinsic analeptic activity, but its analeptic action is less efficacious than that of TRH. In mice, it dose-dependently attenuates the TRH-evoked reversal of barbiturate-induced sleeping time. [Glu2]TRH does not possess an intrinsic ACh-stimulatory effect and opposes the cholinergic effect of TRH in the rat CNS. [Glu2]TRH has been reported to have neuroprotective, antidepressant, anticonvulsant, and other activities in the CNS. Many centrally-mediated effects of TRH are shared with [Glu2]TRH, but they may involve different receptors or mechanisms. For example, [Glu2]TRH does not have TSH-releasing activity and does not elevate thyroid-hormone levels. The diastereomer [D-Glu2]TRH is neither an analeptic nor an inhibitor/negative modulator in the context of the analeptic effect and ACh release. [Glu2]TRH may be considered as a negative modulator for the cholinergic effect of TRH in the mouse brain and has the potential to be used as a lead for the development of pharmacological agents to understand the cholinergic mechanisms of TRH's CNS effects.

一般情况下， [Glu2]TRH 多肽 粉末应该保存在-20甚至-70摄氏度. [Glu2]TRH 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

• Nguyen V, Zharikova AD, Prokai-Tatrai K, Prokai L. [Glu2]TRH dose-dependently attenuates TRH-evoked analeptic effect in mice. Brain Res Bull. 2010 Apr 29;82(1-2):83-6. doi: 10.1016/j.brainresbull.2010.02.007. Epub 2010 Feb 24. PMID: 20188155; PMCID: PMC2867048.

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

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。