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LCZ696中间体 |
CAS No.: |
1369773-39-6 |
分子式: |
2C24H29NO5.Ca |
分子量: |
863.08 |
备注: |
中文名称LCZ696中间体中文同义词AHU377钙盐;沙库必曲钙盐;AHU-377钙盐1369773-39-6;HU377钙盐;LCZ696中间体(AHU-377钙盐);(2R,4S)-5-(联苯-4-基)-4-(氨基)-5-(3-羧基-丙酰基氨基)-2甲基-戊酸乙酯钙盐;(2S,4R)-5-(联苯基-4-基)-4-[(3-羧基丙酰基)氨基]-2-甲基戊酸乙酯钙盐(2:1);原研534-06英文名称AHU-377(heMicalciuMsalt)英文同义词AHU-377(heMicalciuMsalt);(alphaR,gammaS)-gamma-[(3-Carboxy-1-oxopropyl)amino]-alpha-methyl-[1,1’-biphenyl]-4-pentanoicacid4-ethylestercalciumsalt(2:1);(2S,4R)-5-(Biphenyl-4-yl)-4-[(3-carboxypropionyl)amino]-2-methylpentanoicacidethylester,calciumsalt(2:1);AHU-377hemicalciumsalt(2:1);Calciumbis(4-{[(1S,3R)-1-([1,1’-biphenyl]-4-ylmethyl)-4-ethoxy-3-methyl-4-oxobutyl]amino}-4-oxobutanoate);LCZ696(valsartan+sacubitril)impurity1;Ethyl(αR,γS)-γ-[(3-carboxy-1-oxopropyl)amino]-α-methyl-[1,1’-biphenyl]-4-pentanoatehemicalciumsalt;(alpharCAS号1369773-39-6分子式C48H56CaN2O10分子量861.04364EINECS号935-847-3相关类别LCZ696中间体;医药中间体;杂质对照品;LCZ696中间体;对照品-杂质对照品;抗高血压;化工原料;原料药及中间体;医药原料;化学试剂;Intermediates;LCZ696;PharmaceuticalIntermediates;lcz696Mol文件1369773-39-6.mol结构式LCZ696中间体性质熔点>140°C(dec.)密度1.24g/cm3at20℃蒸气压0.001Paat20℃储存条件-20°C溶解度DMSO(微溶,加热)、甲醇(微溶)形态粉末颜色白色至米色LogP-0.66-2.9at20℃andpH2-7LCZ696中间体用途与合成方法应用LCZ696中间体是有机合成中间体,可用于实验室研发过程和化工医药合成过程中,主要用于分析化学中沙库比曲药物研发的标准品和对照品。用途沙必利是一种与缬沙坦联合Chemicalbook使用的降压药。这种名为缬沙坦/沙必利的联合药物在试验中被称为LCZ696,并以Entresto品牌销售,是一种治疗心力衰竭的药物。本品用作该药物中间体和杂质对照品,用于药品申报检测等。生物活性Sacubitril(AHU-377)hemicalciumsalt是有效的NEP抑制剂,IC50值为5nM。Sacubitrilhemicalciumsalt是研究心力衰竭药物LCZ696的一个组分。靶点IC50:5nM(NEP)体外研究Sacubitril(AHU-377)isasinglemoleculethatiscomprisedofmolecularmoietiesofvalsartan,anARB,andSacubitrilhemicalciumsalt,aneprilysininhibitor(1:1ratio).Sacubitril(AHU-377)isconvertedbyenzymaticcleavageoftheethylesterintotheactiveneprilysininhibitingmetaboliteLBQ657.TheinactiveNEPiprecursor,Sacubitrilhemicalciumsalt,doesnotinhibitcollagenaccumulationinfibroblastsnorcardiacmyocytehypertrophy.Incardiacfibroblasts,theactiveNEPiLBQ657hadnodiscernibleeffects.Incontrast,LBQ657modestlyinhibitscardiacmyocytehypertrophy.体内研究Inhumans,Sacubitril(AHU-377)(tmax0.5-1.1h)areabsorbedquickly.SacubitrilhemicalciumsaltisconvertedrapidlyintoLBQ657withitstmaxbeingreachedin1.9-3.5h.Meant1/2valuesforthebiologicallyactiveLBQ657is9.9-11.1h.Invehicle-treateddogs,ANFincreasesurinarysodiumexcretionfrom17.3±3.6to199.5±18.4pequivkglmin.ThiseffectispotentiatedsignificantlyinanimalswhichreceiveSacubitril(AHU-377).UrinaryvolumeisalsopotentiatedinanimalswhichreceiveanivadministrationofSacubitril(AHU-377). |
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