代谢

CAS号：1186486-62-3

品名：Evacetrapib;反式-4-[[(5S)-5-[[[3,5-双(三氟甲基)苯基]甲基](2-甲基-2H-四氮唑-5-基)氨基]-2,3,4,5-四氢-7,9-二甲基-1H-1-苯并氮杂卓-1-基]甲基]环己烷羧酸Evacetrapib

中文别名：反式-4-[[(5S)-5-[[[3,5-双(三氟甲基)苯基]甲基](2-甲基-2H-四氮唑-5-基)氨基]-2,3,4,5-四氢-7,9-二甲基-1H-1-苯并氮杂卓-1-基]甲基]环己烷羧酸;

英文别名：LY2484595;trans-4-[[(5S)-5-[[[3,5-Bis(trifluoromethyl)phenyl]methyl](2-methyl-2H-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1H-1-benzazepin-1-yl]methyl]cyclohexanecarboxylicacid;4-[[(5S)-5-[[3,5-bis(trifluoromethyl)phenyl]methyl-(2-methyltetrazol-5-yl)amino]-7,9-dimethyl-2,3,4,5-tetrahydro-1-benzazepin-1-yl]methyl]cyclohexane-1-carboxylicacid;

分子式：C31H36F6N6O2

分子量：638.647

精确质量：638.28

Psa：87.38

UNII号：51XWV9K850

密度：1.40

简介：EvacetrapibwasadrugunderdevelopmentbyEliLilly&Company(investigationalnameLY2484595)thatinhibitscholesterylestertransferprotein(CETP),whichtransfersandtherebyincreaseshigh-densitylipoproteinandlowerslow-densitylipoprotein(CETPinhibitor].Itisthoughtthatmodifyinglipoproteinlevelsmodifiestheriskofcardiovasculardisease.ThefirstCETPinhibitor,torcetrapib,wasunsuccessfulbecauseitincreasedlevelsofthehormonealdosteroneandincreasedbloodpressure,whichledtoexcesscardiaceventswhenitwasstudied.Evacetrapibdoesnothavethesameeffect.WhenstudiedinasmallclinicaltrialinpeoplewithelevatedLDLandlowHDL,significantimprovementswerenotedintheirlipidprofile.

代谢

CAS号：238750-77-1

品名：托舍多特Tosedostat

中文别名：ALPHA-[[(2R)-2-[(1S)-1-羟基-2-(羟基氨基)-2-氧代乙基]-4-甲基-1-氧代戊基]氨基]苯乙酸环戊酯;他达拉非;

英文别名：cyclopentyl(2S)-2-[[(2R)-2-[(1S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl]-4-methylpentanoyl]amino]-2-phenylacetate;CHR2797-Tosedostat;CHR-2797;UNII-KZK563J2UW;

分子式：C21H30N2O6

分子量：406.473

精确质量：406.21

Psa：124.96

密度：1.24

折射率：1.566

简介：CHR-2797isanovelmetalloenzymeinhibitorthatisconvertedintoapharmacologicalactiveacidproduct(CHR-79888)insidecells.CHR-2797exertsantiproliferativeeffectsagainstarangeoftumorcelllinesinvitroandinvivoandshowsselectivityfortransformedovernontransformedcells.Itsantiproliferativeeffectsareatleast300timesmorepotentthantheprototypicalaminopeptidaseinhibitor,Bestatin.

代谢

CAS号：875446-37-0

品名：安塞曲匹Anacetrapib

中文别名：安塞曲匹

英文别名：MK-0859;UNII-P7T269PR6S;(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-[[2-(4-fluoro-2-methoxy-5-propan-2-ylphenyl)-5-(trifluoromethyl)phenyl]methyl]-4-methyl-1,3-oxazolidin-2-one;

分子式：C30H25F10NO3

分子量：637.508

精确质量：637.167

Psa：38.77

UNII号：P7T269PR6S

密度：

简介：Anacetrapib(USAN,pINN;codenamedMK-0859,Merck)isaCETPinhibitorbeingdevelopedtotreathypercholesterolemia(elevatedcholesterollevels)andpreventcardiovasculardisease.

代谢

CAS号：193275-84-2

品名：洛那法尼LONAFARNIB

中文别名：克利贝特.环已双妥明;克利贝特;4-[2-[4-[(11R)-3,10-二溴-8-氯-6,11-二氢-5H-苯并[5,6]环庚并[1,2-b]吡啶-11-基]-1-哌啶基]-2-氧代乙基]-1-哌啶甲酰胺;

英文别名：1-PiperidinecarboxaMide,4-[2-[4-[(11R)-3,10-dibroMo-8-chloro-6;4-{2-[4-(3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidin-1-yl]-2-oxo-ethyl}-piperidine-1-carboxylicacidamide;4-{2-[4-(3,10-dibromo-8-chloro-6,ll-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidin-1-yl]-2-oxo-ethyl}-piperidine-1-carboxylicacidamide;4-[2-[4-[(11R)-3,10-DibroMo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl]-1-piperidinyl]-2-oxoethyl]-1;[14C]-Lonafarnib;LonafarMib;Sarasar;Lonafarnib[usan];(+)-4-[2-[4-(8-chloro-3,10-dibromo-6,11-dihydro-5H-benzo-[5,6]cyclohepta[1,2-b]-pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyt]-1-piperidinecarboxamide;

分子式：C27H31Br2ClN4O2

分子量：638.822

精确质量：636.05

Psa：79.53

密度：1.536

沸点：710.4ºC at 760mmHg

闪点：383.5ºC

信号词：Warning

危险性防范说明：P305 + P351 + P338

危险标志：GHS07

危险性描述：H315; H319; H335

简介：Lonafarnibisafarnesyltransferaseinhibitor(FTI)thatisbeinginvestigatedinahumanclinicaltrialasapotentialtreatmentforprogeria.