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曲前列尼爾 |
| CAS No.: |
81846-19-7 |
| 分子式： |
C23H34O5 |
| 分子量： |
390.51 |
| 備注： |
中文名稱曲前列尼爾中文同義詞曲羅尼爾;曲前列環(huán)素;曲前列尼爾(瑞莫杜林);曲前列尼爾(瑞莫杜林)1G;曲前列尼爾中間體1;曲前列尼爾;瑞莫杜林;曲前列環(huán)素/曲前列尼爾英文名稱Treprostinil英文同義詞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號81846-19-7分子式C23H34O5分子量390.51EINECS號808-233-7相關(guān)類別醫(yī)藥原料藥;孤兒藥、前列腺素;化工原料;醫(yī)藥原料;貝爾卡主打;Aromatics;ChiralReagents;Intermediates&FineChemicals;PharmaceuticalsMol文件81846-19-7.mol結(jié)構(gòu)式曲前列尼爾性質(zhì)熔點(diǎn)121-123°沸點(diǎn)587.1±50.0°C(Predicted)密度1.158±0.06g/cm3(Predicted)儲存條件Sealedindry,Storeinfreezer,under-20°C溶解度可溶于氯仿（略微加熱）、甲醇（略微加熱）酸度系數(shù)(pKa)3.19±0.10(Predicted)形態(tài)固體顏色灰白色至米色I(xiàn)nChIKeyPAJMKGZZBBTTOY-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曲前列尼爾用途與合成方法理化性質(zhì)曲前列尼爾是是一個(gè)化學(xué)分子式，同時(shí)也是一種藥品。曲前列尼爾主要通過直接舒張肺和全身動(dòng)脈血管床并抑制血小板聚集發(fā)揮作用。概述2002年美國批準(zhǔn)曲前列環(huán)素皮下注射可用于肺動(dòng)脈高壓的治療，2006年得到歐盟批準(zhǔn)，2004年靜脈輸注曲前列環(huán)素治療肺動(dòng)脈高壓也在美國得到了批準(zhǔn)。生物活性Treprostinil(LRX-15)是高效的DP1和EP2激動(dòng)劑，其EC50值分別為0.6±0.1和6.2±1.2nM。靶點(diǎn)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)體外研究TreprostinilhashChemicalbookighaffinityfortheDP1,EP2andIPreceptors(Ki=4.4,3.6and32nM,respectively),lowaffinityforEP1andEP4receptorsandevenloweraffinityforEP3,FPandTPreceptors.ActivationofIP,DP1andEP2receptors,aswithtreprostinil,canallresultinvasodilatationofhumanpulmonaryarteries.Treprostinilinhibitsviabilityofculturedendothelialcolonyformingcells.EndothelialcolonyformingcellsproliferationisstimulatedbyconditionedmediafromTreprostinilpretreatedmesenchymalstemcells.體內(nèi)研究Inhaledtreprostinilsodium,aprostacyclinanalog,isthemostrecentagenttoreceiveFDAapprovalforthetreatmentofafatalorphandisease:pulmonaryarterialhypertension(PAH).Treprostinilpreservesthesinusoidalendothelialcellliningandreducesplateletdepositionearlypost-transplantationcomparedtoplacebo.Hepatictissuebloodflowissignificantlycompromisedintheplacebogroup,whereastreprostinilmaintainsbloodflowsimilartonormallevels.Treprostiniltreatmentsignificantlyincreasesthevessel-formingabilityofendothelialcolonyformingcellscombinedwithmesenchymalstemcellsinMatrigelimplantedinnudemice.SilencingVEGF-Ageneinmesenchymalstemcellsalsoblocksthepro-angiogeniceffectofTreprostinil.TreprostinilismostefficaciousinraisingintracellularcAMPlevelsinmurineandhumanhematopoieticstemandprogenitorcells.TreatmentwithTreprostinilsignificantlyreducestherecruitmentofcellscomparedtonormoxicmice.Treprostinilalsoreducesrightventricularsystolicpressureandslightlyreducesthevascularremodellingbutfailstoreversetherightventricularhypertrophy. |
| 結(jié)構(gòu)式： |
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聯(lián)系人： |
金經(jīng)理 |
地 址： |
湖北省武漢市東湖新技術(shù)開發(fā)區(qū)光谷大道03號 |
郵 編： |
430000 |
電 話： |
18995560451 |
手 機(jī)： |
15102708508 |
傳 真： |
18995560451 |
Q Q： |
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www.hbdhchem.com |
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709783996@qq.com |
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