EptifibatideYog cov antipatelet sib txuas uas yog rau qeb ntawm glycoprotein iib / iiia inhibitors. Nws yog ib qho me me molecule compound nrog cov molecular hnyav thiab cov khoom me me me me. Nws yog dawb lossis yuav luag dawb hmoov lossis crystalline khoom. Molecular Cov Qauv Molecular C35H49N11O9S2, CAS 188627-80-7. Kev nthuav tawm hluav taws xob sib txawv raws li cov xwm txheej sib txawv. Tom qab ua rau hauv dej, nws kev coj ua yuav nce ntxiv. Nws kuj yog siv rau cov neeg mob nrog lub siab ntaiv myocardial infarction (stemi). Nws tuaj yeem siv ua ke nrog cov tshuaj uas tsis txaus siab (xws li cov tshuaj txhuam hniav lim dej) los txhim kho kev tawg ntshav thiab rov qab cov ntshav ntshav. Nws tuaj yeem siv rau kev kho mob ntawm cov neeg mob uas tsis yog Cegment Of for of myocardial infarction (zes myocri) thiab tsis khov angina (UA). Nws txo qis lossis tiv thaiv myocardial ischemia los ntawm kev thaiv platelet kev sib sau ua ke thiab txo qhov tsim cov ntshav txhaws.
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Customized raj yas thiab corks:
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Tshuaj Cov Qauv |
C35H49N11O9S2 |
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Muaj pes tsawg leej |
831 |
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Molecular hnyav |
832 |
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m/z |
831 (100.0%), 832 (37.9%), 833 (9.0%), 833 (7.0%), 832 (4.1%), 834 (3.4%), 833 (1.8%), 832 (1.6%), 833 (1.1%) |
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Kev Ntsuam Xyuas |
C, 50.53; H, 5.94; N, 18.52; O, 17.31; S, 7.71 |
Eptifibatideyog Iib / IIia receptor antagonist uas tau khi tshwj xeeb rau ntawm cov ntshav platelets, thaiv cov kev khi ntawm fibrinogen rau cov receptors no.
1. Inhibition ntawm platelet kev sib sau ua ke: Platelelet kev sib cais yog ib qho ntawm cov kauj ruam tseem ceeb hauv kev tsim cov ntshav txhaws. Iib / IIIA ແ inກ tsev yog cov tseem ceeb hauv platelet sib txuas ntawm cov plategerse, yog li txhawb kev sib txuas platelet sib txuas thiab thromomosis. Los ntawm kev sib tw sib tw rau iib / iiia receptors, nws txwv tsis pub platelelet kev sib cais thiab cuam tshuam tsim.
3. Pharcacokinetics: ib nrab- lub neej nyob hauv lub cev yog hais txog 2.5 teev, feem ntau yog lub raum metabolism thiab kev ua yeeb yam. Vim nws cov lus luv - kev sib txuam, nws feem ntau yog tswj hwm kev pom zoo li cas tsis yog qhov ncauj lus.
2. Kev thim rov qab: Cov nyhoo antiptatelet tau thim rov qab. Thaum txiav tawm, cov tshuaj yuav yog metabolized thiab excreted, thiab platelet ua haujlwm yuav maj mam rov qab mus rau ib txwm. Qhov kev thim rov qab no ua rau upiibati pab tau muaj txiaj ntsig zoo heev - Lub zog yuav tsum tau siv, xws li hauv cov neeg mob myocardial uas cuam tshuam nrog kev cuam tshuam coronary (PCI).
4. Cov nyhuv antithroomic: Cov nyhuv tshuaj antithbic ua rau nws muaj txiaj ntsig hauv ntau qhov kev kho mob. Nws yog dav siv nyob rau hauv cov neeg mob nrog tus mob coronary syndrome (ACS), myocardial infarction (miocardial
5. Kev Nyab Xeeb: Txawm tias Epifiibatid tuaj yeem tiv thaiv cov thromomosis, nws tseem muaj kev pheej hmoo los ntshav. Yog li ntawd, thaum lub sij hawm siv cov tshuaj Epifiibatid, cov neeg ua haujlwm kho mob yuav tsum saib xyuas tus neeg mob kev ua haujlwm sib xyaw, xyuam xim rau qee qhov ua tau los ntshav, thiab coj kev ntsuas. Ib qho ntxiv, nws yuav siv tsis tau nyob hauv qee qhov xwm txheej tshwj xeeb, xws li los ntshav, tswj tsis tau ntshav siab, thiab lwm yam.
6. Kev sib cuam tshuam yeeb tshuaj: Tej zaum muaj kev cuam tshuam nrog lwm cov tshuaj, tshwj xeeb yog cov uas cuam tshuam kev ua haujlwm los ntawm kev sib xyia thiab kev sib cais. Thaum siv cov neeg ua haujlwm Epifiibatid, cov neeg ua haujlwm kho mob yuav tsum tau them sai sai rau lwm cov tshuaj uas tus neeg mob siv thiab kho cov tshuaj lossis saib xyuas raws li xav tau.
Lub sim synthesis txoj kev ntawmEptifibatideFeem ntau cuam tshuam nrog ntau cov kauj ruam, suav nrog xaiv cov ntaub ntawv raw, tswj kev ua haujlwm, thiab kev ua kom huv. Muab cov ntsuas hluavtaws hluavtaws hluavtaws hluav taws xob ncaj qha rau Epitibatide:
Firstly, xaiv cov khoom siv raw xws li Trt MPa Oh, h {{0} ome, thiab lwm yam yooj yim uas yuav tsum muaj rau dipeptide synthesis. Xyuas kom meej tias cov khoom tau yuav cov khoom siv raw ua tau raws li cov qauv tshuaj purity los xyuas kom synthesis.
Trt mpa oh thiab h {{{{0} Lys (FMOC) OMe yog siv los ua cov khoom siv los ua cov kua {}} theem synthesis. Cov kauj ruam no feem ntau cuam tshuam nrog kev hloov pauv xws li kev teeb tsa cov pab pawg tiv thaiv, tsis muaj nyiaj, thiab kev tsim cov peptide beptide. Nyob rau hauv synthesis cov txheej txheem, nws yog qhov tsim nyog tswj cov tshuaj tiv thaiv kev mob, thiab lwm yam nqi, kom ntseeg tau tias kev nce qib ntawm cov tshuaj tiv thaiv thiab kev ruaj ntseg ntawm cov khoom.
Tus synthesized dipepride yog condensed nrog lub h- {{{{{{{{{{{}} nh2 tawg. Cov kauj ruam no feem ntau yog cuam tshuam nrog cov pab pawg tiv thaiv FMOC, ua cov hlua Peptide, thiab teeb tsa sab saw hlau tiv thaiv pab pawg. Cov tshuaj tiv thaiv hws yuav tsum tau nqa tawm nyob rau hauv cov xwm txheej tshwj xeeb kom ntseeg tau qhov tseeb ntawm cov qauv khoom lag luam thiab kev txhim kho ntawm cov txiaj ntsig.
Cov synthesized dipepride yog txuas rau cov khoom tau los ntawm cov av tawg kom tsim cov peptide peptescens tag nrho (boc) {{{pro cys (P1) - NH2. Cov tshuaj tiv thaiv thiab kev ua haujlwm nyob rau theem no zoo ib yam li cov hws ntawm cov tshuaj tiv thaiv kev xav tau kom ntseeg tau tias qhov ruaj khov thiab raug ntawm cov khoom.
Hauv kev tiv thaiv kev tiv thaiv peptides, cov pab pawg tiv thaiv ntawm txhua sab saw yuav tsum tau muab tshem tawm thiab yauv tawm ib qho tshuaj tiv thaiv oxidation kom tau txais cov lus kawg uas muaj qhov kawg. Cov kauj ruam no feem ntau cuam tshuam siv cov kua qaub lossis cov kev daws teeb meem alkaline rau kev tsis txaus siab, thiab siv oxidants xws li H2O2 rau oxidation kev tawm tsam. Nyob rau hauv cov txheej txheem ntawm kev zam thiab oxidation, nws yog qhov tsim nyog los tswj cov tshuaj tiv thaiv cov tshuaj tiv thaiv thiab kev ua tsis tiav los ntawm kev ua tsis tiav lossis tsis tiav oxidation.
Purify cov crude ettifabatide khoom kom tshem tawm impurities thiab los ntawm - cov khoom. Txoj kev huv si tuaj yeem raug xaiv raws li qhov xwm txheej tiag tiag, rov qab ua kua rau cov roj ntsha ua kua chev, thiab cov theem siab.
Kev ua haujlwm ntawm kev ntsuas ntawm kev lim epified epiediibatide los ntsuas nws cov kev cia siab tias muaj kev cuam tshuam. Txoj kev txiav txim siab ua si yuav tuaj yeem raug xaiv raws li cov kev xav tau tiag tiag, xws li kev txiav txim siab platelet cov ntshav glycoprotein GP / IIIA referor antagonistic kev ua si. Los ntawm kev ua cov haujlwm ua haujlwm, cov khoom siv pharifiibatide tuaj yeem hloov kho, muab ib qho hauv paus rau kev tshawb fawb tshuaj thiab chaw kuajmom.
Pharmacyamics yog qhov kev tshawb fawb txog kev nqus, kev faib tawm, cov metabolism, thiab kev lees paub (kev hloov kho tshiab) ua cov tshuaj muaj sia thiab lawv cov kev sib txawv ntawm sab hauv qab. It is crucial for understanding drug mechanisms, optimizing dosing regimens, predicting drug interactions, and evaluating drug safety. Etriptide yog ib platelet glycoprotein iib / iiia recitive antagonist siv nyob rau hauv tus mob coronary kev cuam tshuam (PCI) los txo qhov kev pheej hmoo ntawm cov kev pheej hmoo ntawm thrombosis thiab cov xwm txheej plawv. Nws cov khoom siv hluav taws xob tshwj xeeb ua si ib lub luag haujlwm tseem ceeb hauv kev ua kom muaj kev ua haujlwm zoo thiab kev nyab xeeb hauv chaw kuaj mob.
ETROTTIDE yog feem ntau muab los ntawm kev txhaj tshuaj ntawm sab nrauv, yog li nws txoj kev nqus tsis muaj kev cuam tshuam nrog kev nqus cov plab zom mov. Tom qab kev txhaj tshuaj tag nrho, cov tshuaj nkag rau hauv cov hlab ntshav ncaj qha, zam thawj daim pib ua ntej thiab pub cov tshuaj tiv thaiv cov tshuaj hauv cov tshuaj sai sai. Tsis pub dhau 5 feeb tom qab txhaj tshuaj, cov ntshav siab yuav tsum tau mus txog, thiab qhov kev cuam tshuam sai sai rau cov xwm txheej kub ntxhov uas yuav tsum muaj kev cuam tshuam sai heev ntawm platelet sib cais.
Tom qab nkag mus rau cov ntshav, cov tshuaj yuav faib cov ntaub so ntswg sai rau hauv lub cev. Qhov faib tawm ntawm Eptipatide yog kwv yees li 185ml / kg, uas qhia txog kev faib tawm thoob plaws hauv lub cev, tab sis tsis cuam tshuam cov hlwb lossis khi nrog lwm cov ntaub so ntswg. Nws faib ib nrab - lub neej tsuas yog 5 feeb, qhia tau sai heev thiab tuaj yeem ncav cuag txhua lub hom phiaj nruab nrab hauv lub sijhawm luv. Nws yog tsim nyog sau cia tias tag nrho cov protein khi tus nqi ntawm cov tshuaj muaj nyob hauv cov ntshav, uas ua rau cov tshuaj uas feem ntau yog cov glycoprotein iib / IIia receptors ntawm platelets.
Cov metabolism ntawm lub cev yog qhov yooj yim kuj yooj yim, feem ntau yog los ntawm kev siv tshuaj tiv thaiv famination los tsim cov khoom siv eptifibatid thiab polar metabolites. Cov metabolites tsis muaj kev ua haujlwm roj ntsha, yog li lawv yuav tsis cuam tshuam nrog cov hluav taws xob cuam tshuam ntawm cov tshuaj ntawm cov tshuaj qub. Lub vev xaib tseem ceeb yog daim siab ntawm daim siab, tab sis cov kev siab tshaj plaws ntawm EPTEFIBATID tsis yog siab, uas pab tswj nws txoj kev xav tau ntev. Tsis tas li ntawd, vim kev ua tsis tiav ntawm cov metabolites, tsis tas yuav txhawj xeeb txog lawv qhov kev lom zem los yog tshuaj lom neeg sib cuam tshuam.
Cov kev ua tiav ntawm Eptibatide muaj ntau yam sib txawv, tsuas yog suav nrog rau lub raum zoo li, ua pa ua pa, thiab quav rau excretion. Ntawm lawv, lub raum ua yog lub ntsiab excretion txoj kev, nyiaj txiag rau txog 71.4% ntawm tag nrho cov tshuaj. Qhov kev tshem tawm siab dua (3.79l / h) ua kom cov tshuaj tsis ua kom muaj kev ruaj khov ntawm cov tshuaj muaj ntshav kom muaj kev xav tau. Nyob rau hauv sib piv, tus nqi ntawm cov tshuaj tshwm sim los ntawm kev ua pa thiab quav muaj feem ntau, tsawg dua 1% thiab 1.5% txoj kev muaj kev cuam tshuam rau cov txheej txheem tshem tawm ntawm ptipatide.
Kev tshem tawm ib nrab - Lub neej yog lub sijhawm uas xav tau kev tshem tawm ib nrab hauv lub cev, thiab yog ib qho ntsuas ntsuas qhov ntsuas tau rau kev ntsuas cov tshuaj. Kev tshem tawm ib nrab - Lub neej ntawm Eptipatide yog 1.13-2.5 teev, qhia tias cov tshuaj muaj sai dua kev tshem tawm hauv lub cev. Cov yam ntxwv ua rau muaj kev cuam tshuam rau kev ua tiav kev kho mob hauv lub sijhawm luv luv thiab ua tiav nws cov khoom siv hluav taws xob, ua kom muaj peev xwm ua rau lub cev muaj peev xwm ua rau lub cev.
Rau cov neeg mob uas tsis muaj raum muaj nuj nqi, hemodialysis muaj kev tshuaj noj tshuaj tshuaj kom meej meej. Etriptide yuav tau tshem tawm ntawm Hemodialysis, uas muab kev nyab xeeb rau cov neeg mob uas muaj lub raum tsis tsim nyog siv etrotide. Thaum lub sijhawm Hemodialysis, cov tshuaj tau lim tawm ntawm lub cev los ntawm kev lim ntshav, yog tsis txhob txo cov tshuaj ntau dhau ntawm cov tshuaj hauv lub cev.
Raws li kev ua kom muaj kev ua kom muaj kev ua kom muaj cua daj cua dub glycoprotein iib / ii ecia refor antagonist, lub chaw muag tshuaj tshwj xeeb tshaj plaws ntawmeptifibatideMuab kev txhawb zog rau nws cov ntawv thov kev dav dav dav dav. Kev tshawb fawb yav tom ntej tuaj yeem tshawb ntxiv cov khoom siv hluav taws xob ntawm Eptipatide ntawm Eptipatide hauv cov neeg muaj kev sib txawv, txhawm rau txhim kho kev ua kom muaj txiaj ntsig zoo, thiab txo qhov kev pheej hmoo ntawm kev phiv. Lub caij no, nrog kev txhim kho tas mus li ntawm kev txhim kho kev siv tshuaj yeeb, kev tshawb fawb thiab kev tshawb fawb tshiab ntau rau kev tiv thaiv thiab kho cov kab mob plawv.
Cim npe nrov: Eptifibatide CAS 188627-80-7, cov neeg muag khoom, chaw tsim khoom, chaw tsim khoom, lag luam, yuav, nqe, loj, rau muag