GS-441524 remdesiviryog ib qho me me molecule, hu ua kev sib tw nucleoside triphosphate inhibitor, qhia muaj zog tiv thaiv kab mob tiv thaiv ntau tus kab mob RNA. Nws tuaj yeem inhibit qhov kev rov ua dua ntawm ntau hom kab mob RNA. GS-441524 yog ib qho me me molecule, hu ua kev sib tw nucleoside triphosphate inhibitor, uas qhia tau hais tias muaj zog tiv thaiv kab mob tiv thaiv ntau tus kab mob RNA. Nws tuaj yeem inhibit qhov kev rov ua dua ntawm ntau hom kab mob RNA. Nws yog ib qho me me molecule nucleoside analogue uas nkag mus rau hauv cov cellular phosphorylation nyob rau hauv qhov kev txiav txim ntawm cell kinases hauv lub cev, tsim ib qho active triphosphate metabolite (NTP). NTP tuaj yeem sib tw nrog ntuj nucleotides hauv lub cev, inhibit RNA polymerase, cuam tshuam nrog RNA replication ntawm feline infectious peritonitis tus kab mob, thiab yog li thaiv cov synthesis ntawm feline kis kab mob peritonitis. Daim ntawv nquag ntawm GS441524, GS441524 triphosphate metabolite (NTP), yog ib yam khoom tseem ceeb hauv intracellular signaling, thiab nws cov qauv analogues sib tw nrog ntuj triphosphate nucleosides los koom rau hauv RNA transcription txheej txheem. GS441524 yog phosphorylated rau hauv nucleoside monophosphate los ntawm cellular kinase thiab tom qab ntawd hloov mus ua ib qho active triphosphate metabolite (NTP). Daim ntawv nquag no tuaj yeem ua tus neeg sib tw ntawm natural triphosphate nucleosides hauv viral RNA synthesis, sib tw nrog cov nucleosides ntuj los koom rau hauv RNA transcription.
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Hais Txog Kev Xa Khoom
Ua tiav kev xa khoom thoob plaws ntiaj teb:
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Tshuaj Formula |
C12H13N5O4 |
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Exact Mass |
291.10 |
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Molecular Luj |
291.27 |
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m/z |
291.10 (100.0%), 292.10 (13.0%), 292.09 (1.8%) |
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Elemental Analysis |
C, 49.48; H, 4.50; N, 24.04; O, 21.97 |
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Thov xa mus rau peb tus qauv kev lag luam lossis COA. Yog tias koj xav tau cov ntsiab lus ntxiv, txais tos hu rau peb qhov muag.
Cov ntaub ntawv ntxiv ntawm cov tshuaj sib xyaw: ntom 1.84 + / - 0.1 g / cm3 (Predicted), Acidity coefficient (pKa) 12.13 ± 0.70 (Predicted)
Txoj kev ntawm synthesizingGS441524 remdesivirnyob rau hauv lub chaw soj nstuam yuav tsum tau ib tug series ntawm cov tshuaj tiv thaiv cov kauj ruam los tsim lub core qauv ntawm lub compound. Cov hauv qab no yog cov lus piav qhia tshwj xeeb ntawm cov qauv kev kuaj sim rau GS441524:
Cov ntaub ntawv pib: Cov ntaub ntawv pib rau kev sib txuas GS-441524 feem ntau yog cov neeg pub khoom noj qab zib, cov neeg pub zaub mov raws li nitrogen, thiab phosphorus raws li cov neeg pub. Cov neeg pub dawb no feem ntau yog siv cov khoom pib hauv tshuaj lom neeg thiab tuaj yeem tau yooj yim tau nyob rau hauv kev kuaj mob.
Kauj ruam 1:
Cov pab pawg tiv thaiv: Ua ntej pib cov tshuaj tiv thaiv tom ntej, qee cov pab pawg ua haujlwm yuav tsum tau tiv thaiv kom tsis txhob cuam tshuam nrog cov kev tshwm sim tom ntej. Cov pab pawg tiv thaiv no tuaj yeem raug tshem tawm raws li cov xwm txheej tshwj xeeb, yog li rov ua haujlwm ntawm cov pab pawg ua haujlwm no.
Kauj ruam 2:
Phosphorylation cov tshuaj tiv thaiv: Cov tshuaj tiv thaiv tseem ceeb rau kev sib txuas GS441524 yog cov tshuaj tiv thaiv phosphorylation. Cov tshuaj tiv thaiv no yuav tsum tau siv cov phosphate pub thiab txuas ntawm phosphate pawg rau nitrogen pawg raws li kev ua ntawm ib qho catalyst. Cov tshuaj tiv thaiv no yog thim rov qab thiab yuav tsum tau siv cov xwm txheej tshwj xeeb los txhawb nws txoj kev vam meej.
Kauj Ruam 3:
Tshem tawm cov pab pawg tiv thaiv: Tom qab ua tiav cov tshuaj tiv thaiv phosphorylation, cov pab pawg tiv thaiv yav dhau los yuav tsum tau muab tshem tawm. Cov txheej txheem no yuav tsum tau siv cov tshuaj tiv thaiv tshwj xeeb kom tsis txhob cuam tshuam rau lwm pawg ua haujlwm.
Kauj Ruam 4:
Kev hloov kho thiab kev ua kom huv: Tom qab ua tiav cov txheej txheem tseem ceeb, qee qhov kev hloov pauv yuav tsum tau txais qhov kawg GS441524 molecule. Cov kev hloov pauv no tuaj yeem hloov qee yam khoom ntawm molecules, xws li nce solubility lossis tshem tawm impurities. Thaum kawg, cov kauj ruam ua kom huv huv yuav tsum tau txais siab -purity GS441524.
Tus cwj pwm thiab kev tsom xam: Tom qab kev sib txuas ntawm GS441524, nws yog ib qho tsim nyog yuav tsum ua tus yam ntxwv thiab txheeb xyuas nws kom paub meej tias nws cov qauv tshuaj thiab purity. Qhov no tuaj yeem ua tiav los ntawm kev tshuaj xyuas xws li nuclear magnetic resonance, huab hwm coj spectrometry, thiab siab - ua kua chromatography.
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Lus Cim: BLOOM TECH (Txij li xyoo 2008), ACHIEVE CHEM-TECH yog lub chaw pabcuam ntawm peb.
Nws tuaj yeem cuam tshuam kev sib txuas ntawm ntau hom kab mob RNA, xws li zoonotic mob hnyav ua pa nyuaj (SARS) tus mob coronavirus, Middle East respiratory syndrome virus, Ebola virus, Lassa fever virus, Junin virus thiab ua pa syncytial tus kab mob, thaum uas qhia cytotoxicity tsawg nyob rau hauv ntau hom ntawm tes. GS441524 rau miv yog qhov kev siv dav tshaj plaws.
GS441524 yog ib qho me me molecule nucleoside analogue nrog cov tshuaj tua kab mob, feem ntau yog siv los kho cov kab mob peritonitis hauv miv. Hauv qab no yog cov ncauj lus kom ntxaws tsom xam ntawm kev ua haujlwm tiv thaiv kab mob ntawm GS441524:
Antiviral spectrum:
GS-441524 muaj broad-spectrum antiviral kev ua haujlwm thiab tuaj yeem cuam tshuam kev rov ua dua ntawm ntau yam kab mob RNA, suav nrog feline infectious peritonitis virus, feline coronavirus, canine parvovirus, porcine reproductive and respiratory syndrome virus, thiab lwm yam. Cov kab mob no yog cov kab mob tseem ceeb ntawm cov kab mob sib kis4 ntawm cov tsiaj, thiab cov tsiaj txhu 4. muab qhov muaj peev xwm kho tau cov kab mob no.
Mechanism ntawm kev ua:
Cov txheej txheem ntawm GS-441524 cov tshuaj tiv thaiv kab mob feem ntau cuam tshuam nrog cov txheej txheem hloov pauv ntawm tus kab mob RNA. GS-441524 tuaj yeem sib tw nrog ntuj nucleotides rau RNA polymerase, yog li thaiv cov synthesis ntawm tus kab mob RNA. Tsis tas li ntawd, GS-441524 tseem tuaj yeem ua rau cov cell apoptosis, yog li ua kom ceev cov kab mob tshem tawm.
Kev ua tau zoo:
Hauv kev sim tshuaj, cov txiaj ntsig kho mob ntawm GS-441524 tau raug txheeb xyuas. Rau feline infectious peritonitis, GS-441524 tuaj yeem txo cov tsos mob zoo thiab txhim kho kev ciaj sia ntawm cov miv mob. Tib lub sijhawm, GS-441524 tseem tuaj yeem tiv thaiv thiab kho lwm yam kab mob ntawm tus tsiaj, xws li canine parvovirus.
4. Kev nyab xeeb:
Kev nyab xeeb ntawm kev siv GS-441524 hauv miv tau kawm dav dav thiab kuaj pom tseeb. Raws li cov ntaub ntawv thiab cov ntaub ntawv uas twb muaj lawm, feem coob ntawm cov neeg mob tsis muaj qhov txawv txav ntawm cov ntshav ntsuas thaum siv. Txawm li cas los xij, tej zaum yuav muaj qee qhov kev mob tshwm sim thaum siv GS-441524, nrog rau qhov mob ntawm qhov chaw txhaj tshuaj. Nws yuav tsum raug sau tseg tias GS-441524 tuaj yeem cuam tshuam kev loj hlob ntawm cov hniav mus tas li hauv cov miv hluas yam tsis muaj kev hloov hniav.
GS-441524, raws li kev cog lus tshuaj tiv thaiv kab mob, nws cov tshuaj reactivity yog lub hauv paus ntawm cov tshuaj lub tswv yim ntawm kev ua, thiab tau muaj kev cuam tshuam loj heev rau kev tsim tshuaj, optimization, cia, thiab daim ntawv thov. Kev nkag siab tob txog cov tshuaj reactivity tsis tsuas yog pab qhia cov lus zais ntawm nws cov tshuaj tiv thaiv kab mob, tab sis kuj tseem muab lub hauv paus tseem ceeb rau kev tswj kom zoo, txhim kho kev ruaj ntseg, thiab kev siv tshuaj kho mob tsim tawm hauv kev tsim tshuaj.
Phosphorylation cov tshuaj tiv thaiv: activation and targeting: Cov tshuaj tiv thaiv tseem ceeb hauv cov hlwb yog phosphorylation, uas yog catalyzed los ntawm cov cellular kinases los hloov cov tshuaj tsis muaj zog rau hauv triphosphate metabolites (NTP) nrog cov tshuaj tiv thaiv kab mob. Phosphorylation tsis tsuas yog txhim kho hydrophilicity, ua rau nws yooj yim dua rau nws nkag mus rau hauv cov cell membranes thiab sib sau ua ke hauv cov hlwb, tab sis kuj ua rau nws muaj kev sib raug zoo rau cov enzymes tseem ceeb lossis cov qauv koom nrog hauv cov kab mob sib kis, xws li RNA polymerase thiab DNA polymerase, los ntawm kev nce nqi tsis zoo. Qhov kev ua kom phosphorylation no ua rau nws lub hom phiaj meej rau cov kauj ruam tseem ceeb ntawm tus kab mob replication, zoo inhibiting tus kab mob replication thiab kis tau tus mob. Nws yog ib qho tsim nyog sau cia tias qhov ua tau zoo thiab qhov tshwj xeeb ntawm cov txheej txheem phosphorylation yog cuam tshuam los ntawm ntau yam xws li hom cellular kinase, tshuaj concentration, thiab cellular ib puag ncig (xws li pH thiab ion zog), uas yuav tsum tau ua tiav hauv kev tsim tshuaj thiab kev siv tshuaj kho mob.
Kev sib tw nrog ntuj nucleotides: Cov qauv tsim ua rau nws simulate ntuj nucleotides thiab sib tw khi nrog RNA polymerase khi qhov chaw. Cov txheej txheem no txo qis kev rov ua dua ntawm tus kab mob RNA los ntawm kev cuam tshuam nrog nws cov txheej txheem hloov pauv ib txwm, yog li inhibiting viral proliferation. Nws yog tsim nyog sau cia tias qhov kev khi ntawm cov tshuaj no rau RNA polymerase kuj tseem tuaj yeem ua rau muaj kev hloov pauv hauv cov polymerase, ntxiv rau inhibiting nws cov catalytic. Qhov no ntxiv inhibitory nyhuv txhim kho cov nyhuv antiviral ntawm cov tshuaj. Txawm li cas los xij, nws txoj kev sib raug zoo rau RNA polymerase thiab nws cov qib ntawm kev cuam tshuam ntawm polymerase conformation yog cuam tshuam los ntawm ntau yam, nrog rau cov tshuaj concentration, polymerase hom, cellular ib puag ncig, thiab lwm yam. Cov yam tseem ceeb no yuav tsum tau ua tib zoo soj ntsuam nyob rau hauv cov txheej txheem ntawm kev tshuaj ntsuam tshuaj thiab optimization.
Hydrolysis tshuaj tiv thaiv: kev sib tw stability:Nyob rau hauv cov xwm txheej tshwj xeeb (xws li ib puag ncig acidic), cov tshuaj tiv thaiv hydrolysis nquag tshwm sim, ua rau cov tshuaj tawg mus rau hauv lawv cov amino acids los yog cov khoom me me. Cov tshuaj tiv thaiv hydrolysis tsis tsuas yog txo cov tshuaj purity, tab sis kuj tseem cuam tshuam rau nws cov tshuaj tiv thaiv kab mob thiab bioavailability. Yog li ntawd, thaum lub sij hawm cia, tsheb thauj mus los, thiab siv, yuav tsum nruj me ntsis tswj ib puag ncig tej yam kev mob (xws li pH nqi, kub, av noo) kom txo tau qhov tshwm sim ntawm hydrolysis tshuaj. Tsis tas li ntawd, ua kom muaj kev ruaj ntseg ntawm cov tshuaj los ntawm kev hloov kho tshuaj xws li esterification, amidation, thiab lwm yam kuj yog ib lub tswv yim zoo los daws cov teeb meem hydrolysis.
Oxidation cov tshuaj tiv thaiv: photosensitivity thiab huab cua stability:rhiab heev rau lub teeb thiab oxygen nyob rau hauv cov huab cua, nws yog nquag mus rau oxidative degradation, ua rau cov kev hloov nyob rau hauv cov qauv tshuaj thiab poob ntawm kev ua ntawm cov tshuaj. Oxidation cov tshuaj tiv thaiv tsis tsuas yog txo cov purity, tab sis kuj tseem tuaj yeem tsim cov khoom puas tsuaj, ua rau muaj kev hem thawj rau kev nyab xeeb thiab kev ua tau zoo ntawm cov tshuaj. Yog li ntawd, kev zam lub teeb nruj, kev sib khi, thiab kev ntsuas tshuaj tiv thaiv antioxidant yuav tsum tau ua thaum lub sijhawm tsim khoom, ntim khoom, kev thauj mus los, thiab siv los ua kom muaj kev ruaj ntseg thiab kev nyab xeeb ntawm cov tshuaj.
Lwm yam cuam tshuam:Ntxiv nrog rau cov tshuaj tiv thaiv tseem ceeb uas tau hais los saum no, cov khoom siv tshuaj lom neeg kuj cuam tshuam los ntawm ntau yam xws li tshuaj concentration, hom hnyav, pH regulator, ionic zog, thiab kub. Cov kev hloov pauv hauv cov xwm txheej no tuaj yeem ua rau muaj kev hloov pauv hloov pauv hauv cov khoom siv tshuaj lom neeg, uas cuam tshuam rau lawv cov tshuaj tiv thaiv kab mob thiab kev nyab xeeb. Yog li ntawd, nyob rau hauv cov txheej txheem ntawm kev tsim tshuaj thiab kev siv tshuaj, nws yog ib qho tsim nyog yuav tsum tau ua nyob rau hauv - kev tshawb fawb tob txog cov xwm txheej no txhawm rau txhim kho cov qauv tshuaj thiab kev cia khoom, kom ntseeg tau tias muaj txiaj ntsig thiab kev nyab xeeb ntawm cov tshuaj.
Nyob rau hauv cov ntsiab lus, cov tshuaj reactivity ntawm GS-441524 yog ib tug complex thiab multifaceted teb, npog ntau yam xws li phosphorylation, kev sib tw nrog ntuj nucleotides, hydrolysis, thiab oxidation. Cov yam ntxwv no sib sau ua ke txiav txim siab txog daim ntawv thov thiab kev ceev faj hauv kev kho mob antiviral. Txhawm rau kom ua tiav nws cov tshuaj tiv thaiv kab mob, nws yog ib qho tsim nyog yuav tsum tau ua qhov kev tshawb fawb tob txog nws cov tshuaj reactivity thiab cuam tshuam cov yam ntxwv, txhim kho cov tshuaj formulations thiab cia tej yam kev mob, los xyuas kom meej kev nyab xeeb thiab kev ua tau zoo ntawm cov tshuaj. Lub caij no, kev tshawb fawb yav tom ntej yuav tsum tau tshawb nrhiav cov tswv yim rau kev siv ua ke nrog lwm cov tshuaj tiv thaiv kab mob txhawm rau txhim kho cov tshuaj tiv thaiv kab mob thiab txo cov kev pheej hmoo ntawm cov tshuaj tiv thaiv.
Lub discovery keeb kwm ntawmGS-441524 remdesivirtuaj yeem taug qab rov qab rau xyoo 2012, thaum cov kws tshawb fawb ntawm Gilead Sciences tau tshawb pom ib qho chaw hu ua GS-441524 thaum kawm txog cov txheej txheem rov ua dua ntawm tus kab mob siab C (HCV). Cov tshuaj no nthuav tawm dav-spectrum antiviral kev ua haujlwm tawm tsam ntau yam kab mob, kab mob, lossis kab mob, suav nrog kab mob siab C, mob npaws, mob khaub thuas A, SARS, norovirus, thiab lwm yam.
Gilead Science tau pib ua hauv - kev tshawb fawb tob ntawm GS-441524, thiab pom tias qhov sib xyaw ua ke muaj kev cuam tshuam zoo heev ntawm tus kabmob tshiab (SARS CoV) hauv vitro kev sim. Tom qab ntawd, Gilead Science tau pib tsim GS-441524 ua cov tshuaj kho mob tiv thaiv kab mob siab C thiab tus kab mob tshiab.
Txawm li cas los xij, GS-441524 tsis tau txais kev pom zoo ua cov tshuaj raug cai hauv ib lub tebchaws thoob ntiaj teb. Txawm li cas los xij, Gilead Science tau pub nyiaj ntau ntawm GS-441524 rau Tuam Tshoj rau kev kho tus mob coronavirus tshiab thaum muaj xwm txheej ceev.
Zuag qhia tag nrho, qhov kev tshawb pom keeb kwm ntawm GS-441524 tuaj yeem raug ntaus nqi los ntawm kev tshawb pom thiab kev tshawb fawb ntawm ib qho kev sib txuas nrog dav-spectrum antiviral peev xwm. Txawm hais tias cov tshuaj tseem tsis tau pom zoo, nws tau siv los kho tus mob coronavirus tshiab thiab lwm yam kab mob kis nyob rau qee qhov xwm txheej tshwj xeeb.
FAQ
Puas yog remdesivir zoo ib yam li GS-441524?
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GS-441524 yog cov metabolite ntawm cov tshuaj tiv thaiv kab mob remdesivir(GS-5734) tau siv los kho cov neeg uas muaj tus kab mob SARS-CoV-2, thiab ob qho tshuaj tau txais tib yam metabolite hauv lub cell cell.
GS-441524 puas ua haujlwm?
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Kev kho mob tag nrho yog 84.6%. Tus nqi no tau siab dua thaum GS-441524 tau ua ke nrog lwm cov tshuaj tiv thaiv kab mob thiab qis dua hauv cov ntaub ntawv ntub dej FIP lossis cov neeg muaj teeb meem neurological. Kev sib xyaw ua ke nrog lwm cov tshuaj tiv thaiv kab mob tuaj yeem txhim kho cov txiaj ntsig hauv FIP nyuaj, txawm tias xav tau kev tshawb fawb ntxiv.
Lub npe tshiab rau remdesivir yog dab tsi?
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VEKLURY yog ib hom tshuaj uas siv los kho COVID-19 rau cov neeg laus thiab menyuam yaus uas hnyav li 3 phaus uas tau mus pw hauv tsev kho mob; lossis tsis tau mus pw hauv tsev kho mob thiab muaj mob me me- mus rau nruab nrab COVID-19, thiab muaj kev pheej hmoo siab rau kev kis mus rau COVID-19 hnyav, suav nrog kev mus pw hauv tsev kho mob lossis tuag.
GS-441524 sawv cev rau dab tsi?
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GS-441524 yog anucleoside analogue tshuaj tua kab mobuas yog tsim los ntawm Gilead Sciences. Nws yog lub ntsiab plasma metabolite ntawm antiviral prodrug remdesivir, thiab muaj ib nrab -lub neej nyob ib ncig ntawm 24 teev nyob rau hauv tib neeg cov neeg mob.
Kev kho tshiab rau miv nrog FIP yog dab tsi?
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Ib qho tshuaj sib xyaw ntawm qhov ncauj remdesivir npaj (capsule form)tau siv tau zoo los kho miv nrog FIP thaum GS-441524 tsis muaj, piv txwv li hauv New Zealand (Renner li al., 2025). Molnupiravir (EIDD-2801) yog lwm nucleoside analogue uas inhibits viral replication thiab metabolised rau hauv EIDD-1931 (NHC).
Cim npe nrov: gs-441524 remdesivir cas 1191237-69-0, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom