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曲前列尼尔 |
| CAS No.: |
81846-19-7 |
| 分子式： |
C23H34O5 |
| 分子量： |
390.51 |
| 备注： |
中文名称曲前列尼尔中文同义词曲罗尼尔;曲前列环素;曲前列尼尔(瑞莫杜林);曲前列尼尔(瑞莫杜林)1G;曲前列尼尔中间体1;曲前列尼尔;瑞莫杜林;曲前列环素/曲前列尼尔英文名称Treprostinil英文同义词2-[[[(1R,2R,3aS,9aS)-2α-Hydroxy-1β-[(S)-3-hydroxyoctyl]-2,3,3a,4,9,9a-hexahydro-1H-benzo[f]indene]-5-yl]oxy]aceticacid;UT-15;[[(1R,2R,3aS,9aS)-2,3,3a,4,9,9a-Hexahydro-2-hydroxy-1-[(3S)-3-hydroxyoctyl]-1H-benz[f]inden-5-yl]oxy]aceticacid;Treprostinil-13C2-d1;Treprostinilfreeacid;BW15AU;BW15AU;LRX15;RUMODOLIN;U-62840;UNIPROST;LRX15CAS号81846-19-7分子式C23H34O5分子量390.51EINECS号808-233-7相关类别医药原料药;孤儿药、前列腺素;化工原料;医药原料;贝尔卡主打;Aromatics;ChiralReagents;Intermediates&FineChemicals;PharmaceuticalsMol文件81846-19-7.mol结构式曲前列尼尔性质熔点121-123°沸点587.1±50.0°C(Predicted)密度1.158±0.06g/cm3(Predicted)储存条件Sealedindry,Storeinfreezer,under-20°C溶解度可溶于氯仿（略微加热）、甲醇（略微加热）酸度系数(pKa)3.19±0.10(Predicted)形态固体颜色灰白色至米色InChIKeyPAJMKGZZBBTTOY-ZFORQUDYSA-NSMILESC(O)(=O)COC1=C2C(=CC=C1)C[C@@]1([H])[C@@]([H])(C2)C[C@@H](O)[C@@H]1CC[C@@H](O)CCCCC曲前列尼尔用途与合成方法理化性质曲前列尼尔是是一个化学分子式，同时也是一种药品。曲前列尼尔主要通过直接舒张肺和全身动脉血管床并抑制血小板聚集发挥作用。概述2002年美国批准曲前列环素皮下注射可用于肺动脉高压的治疗，2006年得到欧盟批准，2004年静脉输注曲前列环素治疗肺动脉高压也在美国得到了批准。生物活性Treprostinil(LRX-15)是高效的DP1和EP2激动剂，其EC50值分别为0.6±0.1和6.2±1.2nM。靶点DP/DP1Receptor0.6nM(EC50)IPReceptor1.9nM(EC50)EP2Receptor6.2nM(EC50)EP3Receptor68.9nM(EC50)EP4Receptor181nM(EC50)EP1Receptor285nM(EC50)TPReceptor919nM(EC50)EP2Receptor3.6nM(Ki)EP1Receptor212nM(Ki)EP4Receptor826nM(Ki)EP3Receptor2505nM(Ki)DP/DP1Receptor4.4nM(Ki)IPReceptor32.1nM(Ki)FPReceptor4680nM(Ki)体外研究TreprostinilhashChemicalbookighaffinityfortheDP1,EP2andIPreceptors(Ki=4.4,3.6and32nM,respectively),lowaffinityforEP1andEP4receptorsandevenloweraffinityforEP3,FPandTPreceptors.ActivationofIP,DP1andEP2receptors,aswithtreprostinil,canallresultinvasodilatationofhumanpulmonaryarteries.Treprostinilinhibitsviabilityofculturedendothelialcolonyformingcells.EndothelialcolonyformingcellsproliferationisstimulatedbyconditionedmediafromTreprostinilpretreatedmesenchymalstemcells.体内研究Inhaledtreprostinilsodium,aprostacyclinanalog,isthemostrecentagenttoreceiveFDAapprovalforthetreatmentofafatalorphandisease:pulmonaryarterialhypertension(PAH).Treprostinilpreservesthesinusoidalendothelialcellliningandreducesplateletdepositionearlypost-transplantationcomparedtoplacebo.Hepatictissuebloodflowissignificantlycompromisedintheplacebogroup,whereastreprostinilmaintainsbloodflowsimilartonormallevels.Treprostiniltreatmentsignificantlyincreasesthevessel-formingabilityofendothelialcolonyformingcellscombinedwithmesenchymalstemcellsinMatrigelimplantedinnudemice.SilencingVEGF-Ageneinmesenchymalstemcellsalsoblocksthepro-angiogeniceffectofTreprostinil.TreprostinilismostefficaciousinraisingintracellularcAMPlevelsinmurineandhumanhematopoieticstemandprogenitorcells.TreatmentwithTreprostinilsignificantlyreducestherecruitmentofcellscomparedtonormoxicmice.Treprostinilalsoreducesrightventricularsystolicpressureandslightlyreducesthevascularremodellingbutfailstoreversetherightventricularhypertrophy. |
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