Waxyaabaha ay ka kooban tahay farmashiyaha
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Soodhiyamka Inclisiran
Inclisiran sodium API (Waxyaabaha Farmaceutical Firmaceutical Active) waxaa lagu bartaa ugu horrayn dhanka faragelinta RNA (RNAi) iyo daaweynta wadnaha iyo xididdada dhiigga. Sida siRNA laba-jibbaaran oo lagu beegsanayo hidda-wadaha PCSK9, waxa loo adeegsadaa cilmi-baadhisyo hore iyo kuwo bukaan-socod si loo qiimeeyo xeeladaha aamusinta hidda-wadaha muddada-dheer ee hoos u dhigista LDL-C (kolestaroolka lipoprotein-ka-cufnaanta hoose). Waxa kale oo ay u adeegtaa sidii qaab dhismeed oo loogu talagalay baadhista hababka gudbinta siRNA, xasilloonida, iyo daaweynta RNA ee beerka-la beegsado.
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Fmoc-Gly-Gly-OH
Fmoc-Gly-Gly-OH waa dipeptide loo isticmaalo sidii dhisme aasaasi ah oo ku jira isku-dhafka peptide-wejiga adag (SPPS). Waxay ka kooban tahay laba hadhaaga glycine iyo N-terminus-ilaaliya Fmoc, taas oo u oggolaanaysa dhererka silsiladda peptide ee kontoroolka ah. Sababtoo ah cabbirka yar ee glycine iyo dabacsanaanta, dipeptide-kan waxaa badanaa lagu bartaa macnaha guud ee dhaqdhaqaaqa laf-dhabarka peptide, naqshadeynta isku xirka, iyo qaabeynta qaabdhismeedka peptides iyo borotiinnada.
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Fmoc-Thr(tBu)-Phe-OH
Fmoc-Thr (tBu) -Phe-OH waa dhisme dipeptide ah oo caadi ahaan loo isticmaalo isku-dhafka peptide-wajiga adag (SPPS). Kooxda Fmoc (9-fluorenylmethyloxycarbonyl) waxay ilaalisaa N-terminus, halka kooxda tBu (tert-butyl) ay ilaaliso silsiladda dhinaca hydroxyl ee threonine. Dipeptide-kan la ilaaliyo waxaa lagu daraaseeyaa doorka ay ku leedahay fududaynta fidinta peptide-ka hufan, yaraynta jinsiyada, iyo qaabaynta mawduucyo taxane ah oo gaar ah oo ku saabsan qaabka borotiinka iyo daraasadaha isdhexgalka.
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AEEA-AAEEA
AEEA-AEEA waa hydrophilic, spacer dabacsan oo caadi ahaan loo isticmaalo peptide iyo cilmi-baarista isku xirka daroogada. Waxay ka kooban tahay laba qaybood oo ah ethylene glycol, taas oo ka dhigaysa mid faa'iido u leh barashada saameynta dhererka iskuxiraha iyo dabacsanaanta isdhexgalka molecular, solubility, iyo dhaqdhaqaaqa noolaha. Cilmi-baadhayaashu waxay inta badan isticmaalaan cutubyada AEEA si ay u qiimeeyaan sida spacers u saameeyaan waxqabadka isku-xidhayaasha daawada-antibody-ga (ADCs), conjugates-peptide-daroogada, iyo bioconjugates kale.
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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
Xaruntani waa derivative lysine ah oo la ilaaliyo, shaqaynaysa oo loo isticmaalo isku-dhafka peptide iyo horumarinta isku-xidhka daroogada. Waxay ka kooban tahay kooxda Fmoc ee ilaalinta N-terminal, iyo wax ka beddelka silsiladda dhinaca Eic (OtBu) (eicosanoic acid derivative), γ-glutamic acid (γ-Glu), iyo AEEA (aminoethoxyethoxyacetate). Qaybahan waxaa loogu talagalay in lagu barto saamaynta lipidation-ka, kimistariga spacer-ka, iyo siidaynta daawada la xakameeyey. Waxaa si weyn loo baaraa iyadoo la eegayo istaraatiijiyadaha dawooyinka soo saara, isku xirayaasha ADC, iyo peptides-ka dhex gala xuubabka.
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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
Xaruntani waa derivative lysine ah oo wax laga beddelay oo loo isticmaalo isku-dhafka peptide, gaar ahaan dhisidda isku-xidhayaasha peptide-ka ee la bar-tilmaameedsaday ama hawl-galla. Kooxda Fmoc waxay u oggolaaneysaa isku-dubarid si tartiib tartiib ah iyada oo loo marayo Fmoc solid-phase peptide synthesis (SPPS). Silsiladda dhinaca waxa lagu beddelay derivative stearic acid (Ste), γ-glutamic acid (γ-Glu), iyo laba xidhiidhiye AEEA (aminoethoxyethoxyethoxyacetate), kuwaas oo bixiya hydrophobicity, guryaha dallaca, iyo kala dheerayn dabacsan. Caadi ahaan waxaa lagu daraaseeyaa doorka ay ku leedahay hababka gudbinta daroogada, oo ay ku jiraan isku-xidhayaasha-daawoyinka-anti-body-ga (ADCs) iyo peptides-ka unugyada-gala.
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Boc-His(Trt)-Aib-Gln(Trt)-Gly-OH
Boc-His(Trt)-Aib-Gln(Trt)-Gly-OHwaa tetrapeptide la ilaaliyo oo loo isticmaalo isku dhafka peptide iyo daraasaadka qaabdhismeedka. Kooxda Boc (tert-butyloxycarbonyl) waxay ilaalisaa N-terminus, halka kooxaha Trt (tryl) ay ilaaliyaan silsiladaha dhinaca ee histidine iyo glutamine si ay uga hortagaan falcelinta aan loo baahnayn. Joogitaanka Aib (α-aminoisobutyric acid) waxay kor u qaadaysaa is-waafajinta helical waxayna kor u qaadaysaa xasilloonida peptide. peptide-kani waxa uu qiimo u leeyahay baadhista laalaabida peptide-ka, xasiloonida, iyo qaabaynta peptides noolaha firfircoon.
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Boc-Tyr(tBu)-Aib-Glu(OtBu)-Gly-OH
Boc-Tyr(tBu)-Aib-Glu(OtBu)-Gly-OHwaa tetrapeptide la ilaaliyo oo caadi ahaan loo isticmaalo cilmi baarista isku dhafka peptide. Kooxaha Boc (tert-butyloxycarbonyl) iyo tBu (tert-butyl) waxay u adeegaan sidii kooxo ilaalin ah si ay uga hortagaan falcelinta dhinaca inta lagu guda jiro isu imaatinka silsiladda peptide. Ku darida Aib (α-aminoisobutyric acid) waxay gacan ka geysataa soo saarista qaababka helical iyo kordhinta xasilloonida peptide. Isku xigxiga peptide-kan waxaa lagu daraaseeyaa kartida uu u leeyahay falanqaynta qaabaysan, laalaabida peptide, iyo sidii dhisme dhisme loogu horumarinayo peptides bioactive oo leh xasillooni iyo gaar ahaaneed.
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Fmoc-Ile-Aib-OH
Fmoc-Ile-Aib-OH waa dhisme dipeptide ah oo loo isticmaalo isku-dhafka peptide-wajiga adag (SPPS). Waxay isku daraysaa isoleucine-ilaaliya Fmoc iyo Aib (α-aminoisobutyric acid), oo ah amino acid aan dabiici ahayn oo kor u qaadaya xasilloonida helix iyo iska caabbinta 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
Fmoc-L-Lys[Eic(OtBu)-γ-Glu(OtBu)-AEEA-AEEA] -OH waa dhisme amino acid shaqaynaysan oo loogu talagalay gaarsiinta daroogada la beegsaday iyo bioconjugation. Waxay ka kooban tahay Eic (eicosanoid) moiety isdhexgalka lipid, γ-Glu bartilmaameedka, iyo AEEA spacers ee dabacsanaanta.
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Boc-Tyr(tBu)-Aib-OH
Boc-Tyr(tBu)-Aib-OH waa dhisme dipeptide ah oo la ilaaliyo oo loo isticmaalo isku dhafka peptide, isku darka Boc-protected tyrosine iyo Aib (α-aminoisobutyric acid). Hadhaaga Aib waxa ay xoojisaa samaynta helix iyo iska caabbinta protease.
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Boc-His(Trt)-Ala-Glu(OtBu)-Gly-OH
Boc-His(Trt)-Ala-Glu(OtBu)-Gly-OH waa jajab tetrapeptide ah oo la ilaaliyo oo loo isticmaalo isku dhafka adag ee peptide synthesis (SPPS) iyo horumarinta daroogada peptide. Waxaa ka mid ah kooxaha difaaca ee isku-dhafka orthogonal waxayna soo bandhigaysaa taxane faa'iido u leh naqshadaynta bioactive iyo qaab dhismeedka peptide.