益智二肽

益智二肽化学性质

熔点 :>209°C (dec.)
沸点 :866.2±65.0 °C(Predicted)
密度 :1.111±0.06 g/cm3(Predicted)
储存条件 :Hygroscopic, Refrigerator, under inert atmosphere
溶解度 :DMSO (Slightly), Methanol (Slightly)
形态 :Solid
酸度系数(pKa) :9.83±0.15(Predicted)
颜色 :White to Off-White
序列 :Hexanoyl-Tyr-Ile-Ahx-NH2
InChIKey :ADWKPLXLPNPJTR-JTJYXVOQSA-N
SMILES :C(N)(=O)[C@H]([C@@H](C)CC)N(C(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)CCCCC)CCCCCC(N)=O

益智二肽性质、用途与生产工艺

生物活性 Dihexa (PNB-0408)，一种寡肽试剂，是一种具有口服活性，血脑屏障可渗透性的血管紧张素 IV 类似物。Dihexa 高亲和力结合肝细胞生长因子 (HGF)，Kd 值为 65 pM，并增强了其对受体 c-Met 的活性。Dihexa 在动物模型中显示出优异的抗精神病活性以及改善认知功能。Dihexa 具有研究阿尔茨海默症的潜力。
靶点

Kd: 65 pM (HGF)
体外研究

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.
体内研究

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.
参考质量标准外观:白色粉末
纯度(HPLC) ≥98.0%
醋酸根含量5.0%～12.0%
水分含量≤8.0%
肽含量≥80.0%
氨基酸组成分析≤±10%

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