Ibikoresho bya Farma
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Inclisiran sodium
Inclisiran sodium API (Active Pharmaceutical Ingredient) yizwe cyane cyane mubijyanye no kwivanga kwa RNA (RNAi) hamwe nubuvuzi bwumutima. Nka siRNA ikubye kabiri yibasira gene PCSK9, ikoreshwa mubushakashatsi bwibanze nubuvuzi kugirango isuzume ingamba zimaze igihe zicecekesha gene yo kugabanya LDL-C (cholesterol ya lipoprotein nkeya). Ikora kandi nk'icyitegererezo cyo gukora iperereza kuri sisitemu yo gutanga siRNA, ituze, hamwe na RNA ivura umwijima.
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Fmoc-Gly-Gly-OH
Fmoc-Gly-Gly-OH ni dipeptide ikoreshwa nkigice cyibanze cyubaka muri synthesis ya peptide ikomeye (SPPS). Igaragaza ibisigazwa bibiri bya glycine hamwe na N-terminus irinzwe na Fmoc, ituma urunigi rwa peptide rugenzurwa. Bitewe na glycine ntoya kandi yoroheje, iyi dipeptide ikunze kwigwa murwego rwimikorere ya peptide yingirangingo, igishushanyo mbonera, hamwe no kwerekana imiterere muri peptide na proteyine.
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Fmoc-Thr (tBu) -Phe-OH
Fmoc-Thr (tBu) -Phe-OH ni inyubako ya dipeptide ikunze gukoreshwa muburyo bukomeye bwa peptide ya peptide (SPPS). Itsinda rya Fmoc (9-fluorenylmethyloxycarbonyl) ririnda N-terminus, mugihe itsinda rya tBu (tert-butyl) ririnda hydroxyl kumurongo wa threonine. Iyi dipeptide ikingiwe yizwe kubera uruhare rwayo mu korohereza peptide neza, kugabanya ivanguramoko, no kwerekana imiterere yihariye ikurikirana mu miterere ya poroteyine no mu bushakashatsi bwakozwe.
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AEEA-AEEA
AEEA-AEEA ni hydrophilique, icyogajuru cyoroshye gikoreshwa mubushakashatsi bwa peptide nubushakashatsi bwibiyobyabwenge. Igizwe nibice bibiri bishingiye kuri Ethylene glycol, bituma iba ingirakamaro mukwiga ingaruka zuburebure bwihuza no guhinduka kumikoranire ya molekile, solubile, nibikorwa byibinyabuzima. Abashakashatsi bakunze gukoresha ibice bya AEEA kugirango basuzume uburyo icyogajuru kigira ingaruka kumikorere ya antibody-ibiyobyabwenge (ADCs), peptide-ibiyobyabwenge, nibindi bioconjugate.
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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
Uru ruganda nirinda lysine rukoreshwa, rukoreshwa muri synthesis ya peptide no guteza imbere ibiyobyabwenge. Irimo itsinda rya Fmoc kurinda N-terminal, hamwe no guhindura urunigi kuruhande hamwe na Eic (OtBu) (inkomoko ya acide eicosanoic), acid-glutamic aside (γ-Glu), na AEEA (aminoethoxyethoxyacetate). Ibi bice byateguwe kugirango bige ku ngaruka za lipidation, chimie spacer, no kugenzura ibiyobyabwenge. Irakorwaho ubushakashatsi cyane murwego rwingamba za prodrug, guhuza ADC, na peptide ikorana na 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
Uru ruganda ni lysine yahinduwe ikoreshwa muri synthesis ya peptide, cyane cyane mukubaka peptide ya conjugate cyangwa intego nyinshi. Itsinda rya Fmoc ryemerera guhuza intambwe ikoresheje Fmoc ikomeye-icyiciro cya peptide synthesis (SPPS). Urunigi rwo ku mpande rwahinduwe hamwe na aside ikomoka kuri stearic (Ste), acid-glutamic aside (γ-Glu), hamwe na AEEA (aminoethoxyethoxyacetate) ebyiri, zitanga hydrophobicity, ibintu byishyuza, hamwe n’imyanya yoroheje. Ubusanzwe yizwe kubera uruhare rwayo muri sisitemu yo gutanga ibiyobyabwenge, harimo antibody-ibiyobyabwenge conjugate (ADCs) na peptide yinjira mu ngirabuzimafatizo.
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Boc-We (Trt) -Aib-Gln (Trt) -Gly-OH
Boc-We (Trt) -Aib-Gln (Trt) -Gly-OHni tetrapeptide ikingiwe ikoreshwa muri peptide synthesis hamwe nubushakashatsi bwubatswe. Itsinda rya Boc (tert-butyloxycarbonyl) ririnda N-terminus, mugihe amatsinda ya Trt (trityl) arinda iminyururu yuruhande rwa histidine na glutamine kugirango yirinde kwifata. Kubaho kwa Aib (α-aminoisobutyric aside) biteza imbere guhuza no kongera peptide itajegajega. Iyi peptide ifite agaciro mugukora iperereza rya peptide, itajegajega, kandi nkigishishwa cyo gukora peptide ikora mubuzima.
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Boc-Tyr (tBu) -Aib-Glu (OtBu) -Gly-OH
Boc-Tyr (tBu) -Aib-Glu (OtBu) -Gly-OHni tetrapeptide ikingiwe ikoreshwa mubushakashatsi bwa peptide. Amatsinda ya Boc (tert-butyloxycarbonyl) na tBu (tert-butyl) akora nk'amatsinda arinda amatsinda kugirango akumire ingaruka mugihe cyo guteranya urunigi rwa peptide. Kwinjizamo Aib (α-aminoisobutyric aside) bifasha gutera ibyubaka no kongera peptide itajegajega. Uru ruhererekane rwa peptide rwizwe kubushobozi bwarwo mu isesengura rihuza, gupfunyika peptide, no kuba inyubako yo guteza imbere peptide ya bioaktike ifite imbaraga zihamye kandi zihariye.
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Fmoc-Ile-Aib-OH
Fmoc-Ile-Aib-OH ni dipeptide yubaka ikoreshwa muri synthesis ya peptide ikomeye (SPPS). Ihuza isoleucine irinzwe na Fmoc na Aib (α-aminoisobutyric acide), aside amine idasanzwe karemano yongerera imbaraga za helix no kurwanya 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. Igaragaza icyerekezo cya Eic (eicosanoid) kugirango imikoranire ya lipide, γ-Glu igamije, hamwe na AEEA icyogajuru kugirango ihindurwe.
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Boc-Tyr (tBu) -Aib-OH
Boc-Tyr (tBu) -Aib-OH ni inyubako ya dipeptide irinzwe ikoreshwa muri synthesis ya peptide, ihuza tirozine irinzwe na Boc na Aib (α-aminoisobutyric aside). Ibisigisigi bya Aib byongera imiterere ya helix no kurwanya protease.
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Boc-We (Trt) -Ala-Glu (OtBu) -Gly-OH
Boc-His (Trt) -Ala-Glu (OtBu) -Gly-OH ni agace ka tetrapeptide karinzwe gakoreshwa muri synthesis ya peptide ikomeye (SPPS) no guteza imbere imiti ya peptide. Harimo amatsinda arinda synthèse ya orthogonal kandi agaragaza urukurikirane rwingirakamaro muburyo bwa bioactive na peptide yubatswe.