Lisebelisoa tsa Pharma
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E kenyelletsa sodium
Inclisiran sodium API (Active Pharmaceutical Ingredient) e ithutoa haholo-holo tšimong ea ho kena-kenana le RNA (RNAi) le therapeutics ea pelo. Joalo ka siRNA e nang le likarolo tse peli e shebileng mofuta oa PCSK9, e sebelisoa lipatlisisong tsa pele le tsa bongaka ho lekola maano a nako e telele a ho khutsisa liphatsa tsa lefutso bakeng sa ho theola LDL-C (low-density lipoprotein cholesterol). E boetse e sebetsa e le motsoako oa mohlala bakeng sa ho batlisisa mekhoa ea phepelo ea siRNA, botsitso, le phekolo ea RNA e lebisitsoeng sebeteng.
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Fmoc-Gly-Gly-OH
Fmoc-Gly-Gly-OH ke dipeptide e sebelisoang e le motheo oa moaho ho solid-phase peptide synthesis (SPPS). E na le masala a mabeli a glycine le N-terminus e sirelelitsoeng ke Fmoc, e lumellang ho lelefatsa ketane ea peptide e laoloang. Ka lebaka la boholo bo nyane ba glycine le ho feto-fetoha ha maemo, dipeptide ena hangata e ithutoa maemong a matla a mokokotlo oa peptide, moralo oa lihokela, le sebopeho sa sebopeho ho li-peptide le liprotheine.
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Fmoc-Thr(tBu)-Phe-OH
Fmoc-Thr(tBu)-Phe-OH ke sebaka sa kaho sa dipeptide se atisang ho sebelisoa ho solid-phase peptide synthesis (SPPS). Sehlopha sa Fmoc (9-fluorenylmethyloxycarbonyl) se sireletsa N-terminus, ha sehlopha sa tBu (tert-butyl) se sireletsa ketane ea lehlakore ea hydroxyl ea threonine. Peptide ena e sirelelitsoeng e ithutoa ka karolo ea eona ea ho nolofatsa katoloso e nepahetseng ea peptide, ho fokotsa lebelo la morabe, le ho etsa mohlala oa tatellano e ikhethileng ea sebopeho sa protheine le lithuto tsa tšebelisano.
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AEEA-AEEA
AEEA-AEEA ke hydrophilic, sepakapaka se tenyetsehang se sebelisoang hangata ho lipatlisiso tsa peptide le lithethefatsi. E na le li-unit tse peli tse thehiloeng ho ethylene glycol, e leng se etsang hore e be molemo bakeng sa ho ithuta liphello tsa bolelele ba li-linker le ho feto-fetoha ha litšebelisano tsa limolek'hule, ho qhibiliha, le ts'ebetso ea likokoana-hloko. Hangata bafuputsi ba sebelisa likarolo tsa AEEA ho lekola hore na li-spacers li susumetsa ts'ebetso ea li-antibody-drug conjugates (ADCs), li-conjugate tsa lithethefatsi tsa peptide, le li-bioconjugate tse ling.
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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
Motsoako ona ke motsoako o sirelelitsoeng, o sebetsang oa lysine o sebelisoang ho peptide synthesis le nts'etsopele ea conjugate ea lithethefatsi. E na le sehlopha sa Fmoc bakeng sa tšireletso ea N-terminal, le phetoho ea ketane ea mahlakoreng ka Eic (OtBu) (eicosanoic acid derivative), γ-glutamic acid (γ-Glu), le AEEA (aminoethoxyethoxyacetate). Likarolo tsena li etselitsoe ho ithuta litlamorao tsa lipidation, chemistry ea spacer, le tokollo ea lithethefatsi e laoloang. E batlisisoa haholo molemong oa maano a lihlahisoa, lihokelo tsa ADC, le li-peptide tse sebetsanang le membrane.
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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
Motsoako ona ke motsoako oa lysine o fetotsoeng o sebelisoang ho peptide synthesis, haholo-holo bakeng sa ho aha li-conjugate tsa peptide tse lebisitsoeng kapa tse sebetsang ka bongata. Sehlopha sa Fmoc se lumella ho qaptjoa ha mohato ka mohato ka Fmoc solid-phase peptide synthesis (SPPS). Ketane ea mahlakoreng e fetotsoe ka motsoako oa stearic acid (Ste), γ-glutamic acid (γ-Glu), le lihokelo tse peli tsa AEEA (aminoethoxyethoxyacetate), tse fanang ka hydrophobicity, thepa ea tefiso, le sebaka se feto-fetohang. Hangata e ithutoa ka karolo ea eona litsamaisong tsa phano ea lithethefatsi, ho kenyeletsoa li-antibody-drug conjugates (ADCs) le li-peptide tse kenang liseleng.
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Boc-His(Trt)-Aib-Gln(Trt)-Gly-OH
Boc-His(Trt)-Aib-Gln(Trt)-Gly-OHke tetrapeptide e sirelelitsoeng e sebelisoang ho peptide synthesis le lithuto tsa sebopeho. Sehlopha sa Boc (tert-butyloxycarbonyl) se sireletsa N-terminus, ha lihlopha tsa Trt (trityl) li sireletsa liketane tse ka thōko tsa histidine le glutamine ho thibela liketso tse sa batleheng. Ho ba teng ha Aib (α-aminoisobutyric acid) ho khothalletsa ho lumellana ha helical le ho matlafatsa botsitso ba peptide. Peptide ena e bohlokoa bakeng sa ho etsa lipatlisiso tsa ho mena ha peptide, botsitso, le joalo ka sekhafo sa ho rala li-peptide tse sebetsang ka bioloji.
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Boc-Tyr(tBu)-Aib-Glu(OtBu)-Gly-OH
Boc-Tyr(tBu)-Aib-Glu(OtBu)-Gly-OHke tetrapeptide e sirelelitsoeng eo hangata e sebelisoang liphuputsong tsa peptide synthesis. Lihlopha tsa Boc (tert-butyloxycarbonyl) le tBu (tert-butyl) li sebetsa e le lihlopha tse sireletsang ho thibela maikutlo a mahlakoreng nakong ea kopano ea ketane ea peptide. Ho kenyelletsoa ha Aib (α-aminoisobutyric acid) ho thusa ho etsa hore ho be le mekhoa ea helical le ho eketsa botsitso ba peptide. Tatelano ena ea peptide e ithutoa bakeng sa bokhoni ba eona ba tlhahlobo ea conformational, ho mena ha peptide, le joalo ka moaho oa ho nts'etsapele li-peptide tsa bioactive ka botsitso le boits'oaro bo ntlafalitsoeng.
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Fmoc-Ile-Aib-OH
Fmoc-Ile-Aib-OH ke moaho oa dipeptide o sebelisoang ho solid-phase peptide synthesis (SPPS). E kopanya isoleucine e sirelelitsoeng ea Fmoc le Aib (α-aminoisobutyric acid), e seng ea tlhaho ea amino acid e matlafatsang botsitso ba helix le ho hanyetsa 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 ke mohaho o sebetsang oa amino acid o etselitsoeng ho fana ka lithethefatsi tse lebisitsoeng le bioconjugation. E na le karolo ea Eic (eicosanoid) bakeng sa tšebelisano ea lipid, γ-Glu bakeng sa ho shebisisa, le li-spacers tsa AEEA bakeng sa ho tenyetseha.
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Boc-Tyr(tBu)-Aib-OH
Boc-Tyr(tBu)-Aib-OH ke moaho oa dipeptide o sirelelitsoeng o sebelisoang ho kopantseng peptide synthesis, ho kopanya Boc-protected tyrosine le Aib (α-aminoisobutyric acid). Masala a Aib a matlafatsa sebopeho sa helix le ho hanyetsa protease.
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Boc-His(Trt)-Ala-Glu(OtBu)-Gly-OH
Boc-His(Trt)-Ala-Glu(OtBu)-Gly-OH ke sekhechana se sirelelitsoeng sa tetrapeptide se sebelisoang ho solid-phase peptide synthesis (SPPS) le nts'etsopele ea lithethefatsi tsa peptide. E kenyelletsa lihlopha tse sireletsang bakeng sa orthogonal synthesis mme e fana ka tatellano e sebetsang molemong oa moralo oa peptide oa bioactive le oa sebopeho.