Pharma Izithako
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I-Inclisiran sodium
I-Inclisiran sodium API (I-Active Pharmaceutical Ingredient) ifundwa ngokuyinhloko emkhakheni we-RNA interference (RNAi) kanye nokwelapha kwenhliziyo nemithambo yegazi. Njenge-siRNA enemicu ephindwe kabili eqondise isakhi sofuzo se-PCSK9, isetshenziswa ocwaningweni lwangaphambi kwezempilo nolwezempilo ukuze kuhlolwe amasu asebenza isikhathi eside okuthulisa ufuzo okwehlisa i-LDL-C (low-density lipoprotein cholesterol). Iphinde isebenze njengenhlanganisela yemodeli yokuphenya izinhlelo zokulethwa kwe-siRNA, ukuzinza, kanye nemithi yokwelapha ye-RNA eqondiswe esibindini.
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I-Fmoc-Gly-Gly-OH
I-Fmoc-Gly-Gly-OH iyi-dipeptide esetshenziswa njengebhlokhi yokwakha eyisisekelo ku-solid-phase peptide synthesis (SPPS). Ifaka izinsalela ezimbili ze-glycine kanye ne-Fmoc-protected N-terminus, evumela ukwelulwa kweketango le-peptide elilawulwayo. Ngenxa yobukhulu obuncane be-glycine nokuguquguquka, le dipeptide ivame ukufundwa kumongo we-peptide backbone dynamics, ukwakheka kwe-linker, kanye nokumodela kwesakhiwo kuma-peptide namaprotheni.
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I-Fmoc-Thr(tBu)-Phe-OH
I-Fmoc-Thr(tBu)-Phe-OH iyibhulokhi yokwakha ye-dipeptide evame ukusetshenziswa ku-solid-phase peptide synthesis (SPPS). Iqembu le-Fmoc (9-fluorenylmethyloxycarbonyl) livikela i-N-terminus, kuyilapho iqembu le-tBu (tert-butyl) livikela iketango laseceleni le-hydroxyl le-threonine. Le dipeptide evikelwe icwaningwa ngendima yayo ekusizeni ukunwetshwa kwe-peptide okusebenzayo, ekwehliseni ukugqama kwe-racemization, kanye nokwenza imodeli ye-motif elandelanayo ethile ekwakhekeni kwamaprotheni nezifundo zokusebenzisana.
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AEEA-AEEA
I-AEEA-AEEA iyi-hydrophilic, i-spacer eguquguqukayo evame ukusetshenziswa ocwaningweni lwe-peptide nokuhlanganiswa kwezidakamizwa. Iqukethe amayunithi amabili asekelwe ku-ethylene glycol, okwenza kube usizo ekutadisheni imiphumela yobude besixhumanisi nokuguquguquka ekusebenzisaneni kwamangqamuzana, ukunyibilika, kanye nomsebenzi webhayoloji. Abacwaningi bavame ukusebenzisa amayunithi e-AEEA ukuhlola ukuthi ama-spacers athonya kanjani ukusebenza kwama-antibody-drug conjugates (ADCs), ama-peptide-drug conjugates, namanye ama-bioconjugates.
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![I-Fmoc-L-Lys[Eic(OtBu)-γ-Glu(OtBu)-AEEA]-OH](https://cdn.globalso.com/gentolexgroup/Glepaglutide10-300x300.png)
I-Fmoc-L-Lys[Eic(OtBu)-γ-Glu(OtBu)-AEEA]-OH
Le nhlanganisela iyi-derivative ye-lysine evikelwe, esebenzayo esetshenziswa ekuhlanganiseni kwe-peptide nasekuthuthukisweni kwe-conjugate yezidakamizwa. Ihlanganisa iqembu le-Fmoc lokuvikela i-N-terminal, kanye nokuguqulwa kwe-side-chain nge-Eic(OtBu) (i-eicosanoic acid derivative), γ-glutamic acid (γ-Glu), kanye ne-AEEA (aminoethoxyethoxyacetate). Lezi zingxenye zenzelwe ukutadisha imiphumela ye-lipidation, i-spacer chemistry, nokukhululwa kwezidakamizwa okulawulwayo. Icwaningwa kabanzi kumongo wamasu we-prodrug, izixhumanisi ze-ADC, nama-peptide asebenzisana nolwelwesi.
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![I-Fmoc-L-Lys[Ste(OtBu)-γ-Glu-(OtBu)-AEEA-AEEA]-OH](https://cdn.globalso.com/gentolexgroup/Glepaglutide9-300x300.png)
I-Fmoc-L-Lys[Ste(OtBu)-γ-Glu-(OtBu)-AEEA-AEEA]-OH
Le nhlanganisela iwukuphuma kwe-lysine eguquliwe esetshenziswa ku-peptide synthesis, ikakhulukazi ekwakheni ama-conjugates e-peptide ahlosiwe noma asebenzayo. Iqembu le-Fmoc livumela ukuhlanganiswa kwesinyathelo ngesinyathelo nge-Fmoc solid-phase peptide synthesis (SPPS). Iketango elisemaceleni lilungiswa ngokuphuma kwe-stearic acid (Ste), γ-glutamic acid (γ-Glu), nezixhumi ezimbili ze-AEEA (aminoethoxyethoxyacetate), ezihlinzeka nge-hydrophobicity, izakhiwo zokushaja, nesikhala esivumelana nezimo. Ivamise ukufundelwa indima yayo ezinhlelweni zokulethwa kwezidakamizwa, okuhlanganisa ama-antibody-drug conjugates (ADCs) kanye nama-peptide angena kumaseli.
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I-Boc-His(Trt)-Aib-Gln(Trt)-Gly-OH
I-Boc-His(Trt)-Aib-Gln(Trt)-Gly-OHiyi-tetrapeptide evikelwe esetshenziswa ku-peptide synthesis kanye nezifundo zesakhiwo. Iqembu le-Boc (tert-butyloxycarbonyl) livikela i-N-terminus, kuyilapho amaqembu e-Trt (trityl) avikela amaketanga aseceleni e-histidine ne-glutamine ukuze avimbele ukusabela okungafunwa. Ukuba khona kwe-Aib (α-aminoisobutyric acid) kukhuthaza ukuhlangana kwe-helical futhi kuthuthukise ukuzinza kwe-peptide. Le peptide ibalulekile ekuphenyeni ukugoqeka kwe-peptide, ukuzinza, nanjengesikafula sokuklama ama-peptide asebenza ngokwebhayoloji.
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I-Boc-Tyr(tBu)-Aib-Glu(OtBu)-Gly-OH
I-Boc-Tyr(tBu)-Aib-Glu(OtBu)-Gly-OHiyi-tetrapeptide evikelwe evame ukusetshenziswa ocwaningweni lwe-peptide synthesis. Amaqembu e-Boc (tert-butyloxycarbonyl) kanye ne-tBu (tert-butyl) asebenza njengamaqembu avikelayo ukuze avimbele ukusabela okuseceleni ngesikhathi sokuhlanganisa iketango le-peptide. Ukufakwa kwe-Aib (α-aminoisobutyric acid) kusiza ukuheha izakhiwo ze-helical futhi kwandise ukuzinza kwe-peptide. Lokhu kulandelana kwe-peptide kuhlolwa amandla ako ekuhlaziyeni okuvumelanayo, ukugoqa i-peptide, nanjengesakhiwo sokwakha ama-peptide e-bioactive ngokuzinza nokucaciswa okuthuthukisiwe.
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Fmoc-Ile-Aib-OH
I-Fmoc-Ile-Aib-OH iyibhulokhi yokwakha ye-dipeptide esetshenziswa ku-solid-phase peptide synthesis (SPPS). Ihlanganisa i-isoleucine evikelwe i-Fmoc ne-Aib (i-α-aminoisobutyric acid), i-amino acid engeyona yemvelo ethuthukisa ukuzinza kwe-helix kanye nokumelana ne-protease.
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![I-Fmoc-L-Lys[Eic(OtBu)-γ-Glu(OtBu)-AEEA-AEEA]-OH](https://cdn.globalso.com/gentolexgroup/Glepaglutide6-300x300.png)
I-Fmoc-L-Lys[Eic(OtBu)-γ-Glu(OtBu)-AEEA-AEEA]-OH
I-Fmoc-L-Lys[Eic(OtBu)-γ-Glu(OtBu)-AEEA-AEEA]-OH iyibhulokhi yokwakha esebenzayo ye-amino acid eklanyelwe ukulethwa kwezidakamizwa okuhlosiwe kanye ne-bioconjugation. Ifaka ingxenye ye-Eic (eicosanoid) yokusebenzisana kwe-lipid, i-γ-Glu yokukhomba, kanye nezikhala ze-AEEA zokuguquguquka.
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I-Boc-Tyr(tBu)-Aib-OH
I-Boc-Tyr(tBu)-Aib-OH iyibhulokhi yokwakha ye-dipeptide evikelwe esetshenziswa ekuhlanganiseni kwe-peptide, ehlanganisa i-Boc-protected tyrosine ne-Aib (α-aminoisobutyric acid). Izinsalela ze-Aib zithuthukisa ukwakheka kwe-helix kanye nokumelana ne-protease.
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I-Boc-His(Trt)-Ala-Glu(OtBu)-Gly-OH
I-Boc-His(Trt)-Ala-Glu(OtBu)-Gly-OH iyingxenye evikelwe ye-tetrapeptide esetshenziswa ekuhlanganiseni kwe-peptide synthesis yesigaba esiqinile (SPPS) kanye nokuthuthukiswa kwezidakamizwa ze-peptide. Kuhlanganisa namaqembu okuvikela e-orthogonal synthesis futhi ihlanganisa ukulandelana okuwusizo ekwakhiweni kwe-peptide ye-bioactive kanye nesakhiwo.