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Dihexa(PNB-0408)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Dihexa(PNB-0408)图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Dihexa是一种有口服活性的,可渗透血脑屏障的,血管紧张素IV类似物,对肝细胞生长因子(HGF)具有高亲和力,Kd值为65pM。

Animal experiment:

Rats: Serial dilutions of dihexa in 50% DMSO or water (for dilutions of 50 μg/mL or less) are prepared from the stock used to dose the animals to be used for preparation of a standard curve. 10 μL of each serial dilution is then added to 90 μL of blank plasma for final concentrations of 0.01, 0.02, 0.05, 0.1, 0.2, 1, 10, 20, 50, and 100 μg/mL. 80 μL of each plasma sample is transferred to previously prepared tubes containing 240 μL of ice-cold acetonitrile and vortexed vigorously. 10 μL of isotonic saline containing 100 μg/mL Nle-YI-(6) aminohexanoic amide as an internal standard is added to each sample on ice. The standard-curve plasma samples are then stored at –20℃ and further processed alongside the pharmacokinetic study samples[2].

产品描述

Dihexa is an orally active, blood-brain barrier-permeable angiotensin IV analog; exhibits high affinity binding hepatocyte growth factor (HGF) with a Kd of 65 pM.

Dihexa binds with high affinity to HGF and both dihexa and its parent compound Norleucine 1-AngIV induce c-Met phosphorylation in the presence of subthreshold concentrations of HGF and augment HGF-dependent cell scattering. Further, dihexa and Nle1-AngIV induce hippocampal spinogenesis and synaptogenesis similar to HGF itself. Dihexa effectively inhibits HGF dimerization at 1 μM. While dihexa at 1 nM and 10 pM alone does not activate c-Met, it markedly augments the capacity of HGF at 1.25 and 2.5 ng/mL to activate c-Met[1].

Dihexa has a long circulating half-life. Dihexa exhibits procognitive activity. Dihexa reverses scopolamine-dependent spatial learning deficits. It improves spatial learning in aged rats. Dihexa induces spinogenesis in cultured hippocampal neurons[2].

[1]. Benoist CC, et al. The procognitive and synaptogenic effects of angiotensin IV-derived peptides are dependent on activation of the hepatocyte growth factor/c-met system. J Pharmacol Exp Ther. 2014 Nov;351(2):390-402. [2]. McCoy AT, et al. Evaluation of metabolically stabilized angiotensin IV analogs as procognitive/antidementia agents. J Pharmacol Exp Ther. 2013 Jan;344(1):141-54.