Cov khoom xyaw tshuaj
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Inclisiran sodium
Inclisiran sodium API (Active Pharmaceutical Ingredient) yog kawm feem ntau hauv kev cuam tshuam ntawm RNA (RNAi) thiab kev kho mob plawv. Raws li ob-stranded siRNA lub hom phiaj ntawm PCSK9 noob, nws yog siv nyob rau hauv preclinical thiab soj ntsuam kev tshawb fawb los soj ntsuam cov gene-silencing lub tswv yim ntev rau txo LDL-C (tsawg-density lipoprotein cholesterol). Nws kuj tseem ua haujlwm ua qauv sib xyaw rau kev tshawb xyuas siRNA kev xa khoom, kev ruaj ntseg, thiab lub siab-targeted RNA kho.
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Fmoc-Gly-Gly-OH
Fmoc-Gly-Gly-OH yog ib qho dipeptide siv los ua lub tsev thaiv hauv cov txheej txheem peptide synthesis (SPPS). Nws nta ob glycine residues thiab Fmoc-tiv thaiv N-terminus, tso cai rau kev tswj peptide saw elongation. Vim glycine qhov me me thiab qhov yooj yim, qhov dipeptide no feem ntau tau kawm nyob rau hauv cov ntsiab lus ntawm peptide caj qaum dynamics, linker tsim, thiab cov qauv qauv hauv peptides thiab cov proteins.
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Fmoc-Thr(tBu)-Ph-OH
Fmoc-Thr(tBu)-Phe-OH yog ib lub tsev thaiv dipeptide feem ntau siv hauv cov khoom siv peptide synthesis (SPPS). Fmoc (9-fluorenylmethyloxycarbonyl) pawg tiv thaiv N-terminus, thaum pawg tBu (tert-butyl) tiv thaiv hydroxyl sab saw ntawm threonine. Qhov kev tiv thaiv dipeptide no tau kawm rau nws lub luag haujlwm hauv kev ua kom muaj txiaj ntsig zoo ntawm peptide elongation, txo cov racemization, thiab ua qauv qhia cov qauv tshwj xeeb hauv cov qauv protein thiab kev kawm sib cuam tshuam.
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AEEA-UA
AEEA-AEEA yog hydrophilic, hloov tau yooj yim spacer feem ntau siv nyob rau hauv peptide thiab tshuaj conjugation kev tshawb fawb. Nws muaj ob chav ethylene glycol-based units, ua rau nws muaj txiaj ntsig zoo rau kev kawm txog qhov cuam tshuam ntawm qhov txuas txuas ntev thiab yoog raws ntawm kev sib cuam tshuam ntawm molecular, solubility, thiab lom lom. Cov kws tshawb fawb feem ntau siv AEEA cov chav ntsuas los ntsuas seb cov spacers cuam tshuam li cas ntawm cov tshuaj tiv thaiv kab mob sib txuas (ADCs), peptide-drug conjugates, thiab lwm yam 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
Cov tshuaj no yog ib qho kev tiv thaiv, ua haujlwm tau zoo lysine derivative siv hauv peptide synthesis thiab tshuaj conjugate txoj kev loj hlob. Nws nta ib pab pawg Fmoc rau N-terminal kev tiv thaiv, thiab kev hloov pauv ntawm cov saw txuas nrog Eic (OtBu) (eicosanoic acid derivative), γ-glutamic acid (γ-Glu), thiab AEEA (aminoethoxyethoxyacetate). Cov khoom no yog tsim los kawm txog cov teebmeem lipidation, spacer chemistry, thiab tswj cov tshuaj tso tawm. Nws yog dav tshawb fawb nyob rau hauv cov ntsiab lus ntawm prodrug cov tswv yim, ADC linkers, thiab 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
Cov tshuaj no yog hloov kho lysine derivative siv nyob rau hauv peptide synthesis, tshwj xeeb tshaj yog rau kev tsim lub hom phiaj los yog multifunctional peptide conjugates. Fmoc pab pawg tso cai rau kev sib xyaw ua ke ntawm Fmoc solid-phase peptide synthesis (SPPS). Cov saw hlau sab yog hloov kho nrog stearic acid derivative (Ste), γ-glutamic acid (γ-Glu), thiab ob lub AEEA (aminoethoxyethoxyacetate) txuas, uas muab hydrophobicity, nqi zog, thiab hloov tau yooj yim. Nws feem ntau tau kawm txog nws lub luag haujlwm hauv kev xa tshuaj, suav nrog tshuaj tiv thaiv kab mob-tshuaj yeeb tshuaj (ADCs) thiab cell-peptides.
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Boc-His(Trt)-Aib-Gln(Trt)-Gly-OH
Boc-His(Trt)-Aib-Gln(Trt)-Gly-OHyog ib qho kev tiv thaiv tetrapeptide siv nyob rau hauv peptide synthesis thiab kev tshawb fawb ntawm cov qauv. Cov pab pawg Boc (tert-butyloxycarbonyl) tiv thaiv N-terminus, thaum Trt (trityl) pawg tiv thaiv sab chains ntawm histidine thiab glutamine los tiv thaiv kev tsis haum xeeb. Lub xub ntiag ntawm Aib (α-aminoisobutyric acid) txhawb nqa helical conformations thiab txhim kho peptide stability. Cov peptide no muaj txiaj ntsig zoo rau kev tshawb nrhiav peptide folding, ruaj khov, thiab ua ib qho chaw rau kev tsim cov tshuaj lom neeg peptides.
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Boc-Tyr(tBu)-Aib-Glu(OtBu)-Gly-OH
Boc-Tyr(tBu)-Aib-Glu(OtBu)-Gly-OHyog ib qho kev tiv thaiv tetrapeptide feem ntau siv hauv kev tshawb fawb peptide synthesis. Cov pab pawg Boc (tert-butyloxycarbonyl) thiab tBu (tert-butyl) pab pawg tiv thaiv kom tsis txhob muaj kev cuam tshuam sab nraud thaum lub sij hawm peptide saw sib dhos. Kev suav nrog Aib (α-aminoisobutyric acid) pab txhawb cov qauv helical thiab nce peptide stability. Qhov no peptide sib lawv liag yog kawm rau nws lub peev xwm nyob rau hauv conformational tsom xam, peptide folding, thiab raws li ib tug lub tsev thaiv nyob rau hauv tsim bioactive peptides nrog txhim khu kev ruaj ntseg thiab tshwj xeeb.
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Fmoc-Ile-Aib-OH
Fmoc-Ile-Aib-OH yog dipeptide tsev thaiv siv nyob rau hauv solid-phase peptide synthesis (SPPS). Nws ua ke Fmoc-tiv thaiv isoleucine nrog Aib (α-aminoisobutyric acid), uas tsis yog-natural amino acid uas txhim kho helix stability thiab protease kuj.
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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 yog ib tug functionalized amino acid tsev thaiv tsim rau lub hom phiaj xa tshuaj thiab bioconjugation. Nws nta Eic (eicosanoid) moiety rau lipid kev sib cuam tshuam, γ-Glu rau lub hom phiaj, thiab AEEA spacers rau yooj.
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Boc-Tyr(tBu)-Aib-OH
Boc-Tyr(tBu)-Aib-OH yog lub tsev tiv thaiv dipeptide siv hauv peptide synthesis, combining Boc-tiv thaiv tyrosine thiab Aib (α-aminoisobutyric acid). Aib residue txhim kho helix tsim thiab protease kuj.
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Boc-His(Trt)-Ala-Glu(OtBu)-Gly-OH
Boc-His(Trt)-Ala-Glu(OtBu)-Gly-OH yog ib qho kev tiv thaiv tetrapeptide fragment siv nyob rau hauv solid-phase peptide synthesis (SPPS) thiab peptide tshuaj txhim kho. Nws suav nrog cov pab pawg tiv thaiv rau orthogonal synthesis thiab nta ib ntu muaj txiaj ntsig hauv bioactive thiab cov qauv peptide tsim.