中文名称益智二肽中文同义词益智二肽;化合物DIHEXA;N-((S)-1-(((2S,3S)-1-((6-氨基-6-氧代己基)氨基)-3-甲基-1-氧代戊烷-2-基)氨基)-3-(4-羟基苯基)-1-氧代丙烷-2-基)己酰胺英文名称Dihexa英文同义词Dihexa;Hexanoyl-Tyr-Ile-Ahx-NH2;N-hexanoic-Try-Ile-(6)-aminohexanoicamide;PNB-0408;Dihexa(PNB-0408);N-(1-OXOHEXYL)-L-TYROSYL-N-(6-AMINO-6-OXOHEXYL)-L-ISOLEUCINAMIDE;L-Isoleucinamide,N-(1-oxohexyl)-L-tyrosyl-N-(6-amino-6-oxohexyl)-;TIANFUCHEM--1401708-83-5---DihexaCAS号1401708-83-5分子式C27H44N4O5分子量504.66EINECS号227-005-2相关类别多肽中间体;武汉贝尔卡主打Mol文件1401708-83-5.mol结构式益智二肽性质熔点>209°C(dec.)沸点866.2±65.0°C(Predicted)密度1.111±0.06g/cm3(Predicted)储存条件Hygroscopic,Refrigerator,underinertatmosphere溶解度可溶于DMSO(少许)、甲醇(少许)形态固体酸度系数(pKa)9.83±0.15(Predicted)颜色白色至类白色序列Hexanoyl-Tyr-Ile-Ahx-NH2InChIKeyADWKPLXLPNPJTR-JTJYXVOQSA-NSMILESC(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益智二肽用途与合成方法生物活性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Chemicalbook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65pM,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:65pM(HGF)体外研究DihexabindswithhighaffinitytoHGFandbothdihexaanditsparentcompoundNorleucine1-AngIVinducec-MetphosphorylationinthepresenceofsubthresholdconcentrationsofHGFandaugmentHGF-dependentcellscattering.Further,dihexaandNle1-AngIVinducehippocampalspinogenesisandsynaptogenesissimilartoHGFitself.DihexaeffectivelyinhibitsHGFdimerizationat1μM.Whiledihexaat1nMand10pMalonedoesnotactivatec-Met,itmarkedlyaugmentsthecapacityofHGFat1.25and2.5ng/mLtoactivatec-Met.体内研究Dihexahasalongcirculatinghalf-life.Dihexaexhibitsprocognitiveactivity.Dihexareversesscopolamine-dependentspatiallearningdeficits.Itimprovesspatiallearninginagedrats.Dihexainducesspinogenesisinculturedhippocampalneurons.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% |