Pharma Izithako
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I-Inclisiran sodium
I-Inclisiran sodium API (i-Active Pharmaceutical Ingredient) ifundwa ngokuyinhloko kwintsimi ye-RNA interference (RNAi) kunye ne-cardiovascular therapeutics. Njenge-siRNA ephindwe kabini ejolise kwi-PCSK9 gene, isetyenziselwa uphando lwangaphambili kunye nophando lweklinikhi ukuvavanya izicwangciso zexesha elide zokuthulisa imfuza yokunciphisa i-LDL-C (i-low-density lipoprotein cholesterol). Ikwasebenza njengekhompawundi yemodeli yokuphanda ngeenkqubo zokuhanjiswa kwe-siRNA, uzinzo, kunye nonyango lwe-RNA olujoliswe esibindini.
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Fmoc-Gly-Gly-OH
I-Fmoc-Gly-Gly-OH yidipeptide esetyenziswa njengebhloko yokwakha esisiseko kwi-soli-phase peptide synthesis (SPPS). Ibonisa iintsalela ze-glycine ezimbini kunye ne-Fmoc-ekhuselweyo ye-N-terminus, evumela ukulawulwa kwekhonkco le-peptide. Ngenxa yobungakanani obuncinci be-glycine kunye nokuguquguquka, le dipeptide ihlala ifundwa kumxholo we-peptide backbone dynamics, uyilo lwekhonkco, kunye nemodeli yesakhiwo kwiipeptide kunye neeproteni.
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Fmoc-Thr(tBu)-Phe-OH
I-Fmoc-Thr(tBu)-Phe-OH yibhloko yokwakha yeedipeptide eqhele ukusetyenziswa kwi-soli-phase peptide synthesis (SPPS). Iqela le-Fmoc (i-9-fluorenylmethyloxycarbonyl) likhusela i-N-terminus, ngelixa iqela le-tBu (tert-butyl) likhusela i-hydroxyl side chain of threonine. Le dipeptide ikhuselweyo iphononongwa ngendima yayo ekuququzeleleni ulwalulo olululo lwepeptide, ukunciphisa iracemization, kunye nokwenza imodeli yemotifs yolandelelwano oluthile kulwakhiwo lweprotheyini kunye nezifundo zokusebenzisana.
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AEEA-AEEA
I-AEEA-AEEA yi-hydrophilic, i-flexible spacer edla ngokusetyenziswa kwi-peptide kunye nophando lokudibanisa iziyobisi. Iqukethe iiyunithi ezimbini ezisekelwe kwi-ethylene glycol, okwenza kube luncedo ekufundeni imiphumo ye-linker ubude kunye nokuguquguquka kwintsebenziswano ye-molecular, i-solubility, kunye nomsebenzi we-biological. Abaphandi bahlala besebenzisa iiyunithi ze-AEEA ukuvavanya ukuba i-spacers zinefuthe njani ekusebenzeni kwe-antibody-drug conjugates (ADCs), i-peptide-drug conjugates, kunye nezinye i-bioconjugates.
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![Fmoc-L-Lys[Eic(OtBu)-γ-Glu(OtBu)-AEEA]-OH](https://cdn.globalso.com/gentolexgroup/Glepaglutide10-300x300.png)
Fmoc-L-Lys[Eic(OtBu)-γ-Glu(OtBu)-AEEA]-OH
Le khompawundi lukhuselweyo, lusebenza ngokuphuma kwi-lysine esetyenziswa kwi-peptide synthesis kunye nophuhliso lwe-conjugate yeziyobisi. Ibonisa iqela le-Fmoc lokukhusela i-N-terminal, kunye nokuguqulwa kwe-side-chain kunye ne-Eic (OtBu) (i-eicosanoic acid derivative), i-γ-glutamic acid (γ-Glu), kunye ne-AEEA (aminoethoxyethoxyacetate). La macandelo enzelwe ukufunda iziphumo ze-lipidation, i-spacer chemistry, kunye nokukhutshwa kweziyobisi ezilawulwayo. Iphandwa ngokubanzi kumxholo wezicwangciso zeprodrug, i-ADC linkers, kunye ne-membrane-interacting peptides.
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![Fmoc-L-Lys[Ste(OtBu)-γ-Glu-(OtBu)-AEEA-AEEA]-OH](https://cdn.globalso.com/gentolexgroup/Glepaglutide9-300x300.png)
Fmoc-L-Lys[Ste(OtBu)-γ-Glu-(OtBu)-AEEA-AEEA]-OH
Le khompawundi yi-lysine derivative eguquliweyo esetyenziswa kwi-peptide synthesis, ngakumbi ekwakheni i-conjugates yepeptide ekujoliswe kuyo okanye esebenzayo. Iqela le-Fmoc livumela ukuhlanganiswa kwe-stepwise nge-Fmoc solid-phase peptide synthesis (SPPS). Ikhonkco elisecaleni liguqulwa kunye ne-stearic acid derivative (Ste), γ-glutamic acid (γ-Glu), kunye ne-AEEA (aminoethoxyethoxyacetate) ezimbini zokudibanisa, ezibonelela nge-hydrophobicity, iipropati zentlawulo, kunye ne-flexible spacing. Iqhele ukufundwa ngendima yayo kwiinkqubo zokuhanjiswa kweziyobisi, kubandakanywa i-antibody-drug conjugates (ADCs) kunye neepeptides ezingena kwiseli.
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Boc-His(Trt)-Aib-Gln(Trt)-Gly-OH
Boc-His(Trt)-Aib-Gln(Trt)-Gly-OHyitetrapeptide ekhuselweyo esetyenziswa kwi-peptide synthesis kunye nezifundo zesakhiwo. Iqela le-Boc (tert-butyloxycarbonyl) likhusela i-N-terminus, ngelixa amaqela e-Trt (trityl) akhusela amatyathanga asecaleni e-histidine kunye ne-glutamine ukukhusela ukuphendula okungafunwayo. Ubukho be-Aib (α-aminoisobutyric acid) bukhuthaza ukuhambelana kwe-helical kunye nokuphucula ukuzinza kwe-peptide. Le peptide ixabisekile ekuphandeni ukusonga iipeptide, uzinzo, nanjengesikafula ukuyila iipeptides ezisebenza ngokwebhayoloji.
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I-Boc-Tyr(tBu)-Aib-Glu(OtBu)-Gly-OH
I-Boc-Tyr(tBu)-Aib-Glu(OtBu)-Gly-OHyitetrapeptide ekhuselweyo eqhele ukusetyenziswa kuphando lwe-peptide synthesis. Amaqela e-Boc (tert-butyloxycarbonyl) kunye ne-tBu (tert-butyl) asebenza njengamaqela akhuselayo ukuthintela ukusabela okusecaleni ngexesha lokudityaniswa kwekhonkco le-peptide. Ukufakwa kwe-Aib (α-aminoisobutyric acid) kunceda ukukhupha izakhiwo ze-helical kunye nokwandisa ukuzinza kwe-peptide. Olu landelelwano lwe-peptide lufundelwa amandla alo kuhlalutyo oluhambelanayo, ukusonga i-peptide, kwaye njengebhloko yokwakha ekuphuhliseni iipeptides ze-bioactive kunye nozinzo oluphuculweyo kunye neenkcukacha.
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Fmoc-Ile-Aib-OH
I-Fmoc-Ile-Aib-OH yibhloko yokwakha yeedipeptide esetyenziswa kwi-soli-phase peptide synthesis (SPPS). Idibanisa i-isoleucine ekhuselweyo ye-Fmoc kunye ne-Aib (i-α-aminoisobutyric acid), i-amino acid engeyiyo yendalo eyenza i-helix iqine kunye nokuxhathisa i-protease.
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![Fmoc-L-Lys[Eic(OtBu)-γ-Glu(OtBu)-AEEA-AEEA]-OH](https://cdn.globalso.com/gentolexgroup/Glepaglutide6-300x300.png)
Fmoc-L-Lys[Eic(OtBu)-γ-Glu(OtBu)-AEEA-AEEA]-OH
I-Fmoc-L-Lys [Eic (OtBu)-γ-Glu (OtBu)-AEEA-AEEA] -OH yibhloko yokwakha i-amino acid esebenzayo eyenzelwe ukuhanjiswa kweziyobisi ezijoliswe kuyo kunye ne-bioconjugation. Ibonisa i-Eic (eicosanoid) i-moiety yokusebenzisana kwe-lipid, i-γ-Glu yokujolisa, kunye ne-AEEA spacers yokuguquguquka.
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Boc-Tyr(tBu)-Aib-OH
I-Boc-Tyr(tBu)-Aib-OH yibhloko yokwakha yeedipeptide ekhuselweyo esetyenziswa kwi-peptide synthesis, edibanisa i-Boc-protected tyrosine kunye ne-Aib (α-aminoisobutyric acid). Intsalela ye-Aib yongeza ukubunjwa kwe-helix kunye nokumelana ne-protease.
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Boc-His(Trt)-Ala-Glu(OtBu)-Gly-OH
I-Boc-His (Trt)-Ala-Glu (OtBu)-Gly-OH yiqhekeza le-tetrapeptide elikhuselweyo elisetyenziswe kwi-peptide synthesis yesigaba esiqinileyo (SPPS) kunye nophuhliso lweziyobisi ze-peptide. Ibandakanya amaqela akhuselayo kwi-orthogonal synthesis kunye neempawu zokulandelelana luncedo kwi-bioactive kunye ne-structural peptide design.