Nga Kai Rongoa
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konutai Inclisiran
Ko te Inclisiran sodium API (Active Pharmaceutical Ingredient) e tino akohia ana i roto i te mara o te wawaotanga RNA (RNAi) me nga rongoa cardiovascular. I te mea he siRNA paerua-rua e aro ana ki te ira PCSK9, ka whakamahia i roto i te rangahau haumanu me te rangahau haumanu ki te arotake i nga rautaki whakaheke ira-a-roa mo te whakaheke i te LDL-C (te cholesterol iti-density lipoprotein cholesterol). Ka noho ano hei tauira tauira mo te tirotiro i nga punaha tuku siRNA, te pumau, me nga rongoa RNA e whaaia ana e te ate.
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Fmoc-Gly-Gly-OH
Ko te Fmoc-Gly-Gly-OH he dipeptide e whakamahia ana hei poraka hanga taketake i roto i te whakahiato peptide-waahanga totoka (SPPS). E rua nga toenga glycine me tetahi N-terminus tiaki-Fmoc, e taea ai te whakaroa o nga mekameka peptide. Na te iti o te rahi me te ngawari o te glycine, ka akohia tenei dipeptide i roto i te horopaki o te hihiri o te tuara peptide, te hoahoa hono, me te whakatauira hanganga i roto i nga peptides me nga pūmua.
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Fmoc-Thr(tBu)-Phe-OH
Ko te Fmoc-Thr(tBu)-Phe-OH he poraka hanga dipeptide e whakamahia nuitia ana i roto i te whakahiato peptide-waahanga totoka (SPPS). Ko te roopu Fmoc (9-fluorenylmethyloxycarbonyl) e tiaki ana i te N-terminus, ko te roopu tBu (tert-butyl) e tiaki ana i te mekameka taha hydroxyl o te threonine. Ka rangahaua tenei dipeptide whakamarumaru mo tana mahi ki te whakahaere i te whakaroa peptide pai, te whakaheke i te raemi, me te whakatauira i nga kaupapa raupapa motuhake i roto i te hanganga pūmua me nga rangahau taunekeneke.
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AEEA-AEEA
Ko te AEEA-AEEA he hauwai, he mokowhiti ngawari e whakamahia nuitia ana i roto i te peptide me te rangahau whakakotahitanga tarukino. E rua nga waeine ethylene glycol, e whai hua ana mo te ako i nga paanga o te roa o te hono me te ngawari ki nga tauwhitinga ngota, te whakarewatanga me te mahi koiora. He maha nga wa ka whakamahia e nga Kairangahau nga waeine AEEA ki te arotake i te awe o nga mokowhiti i te mahi o nga whakangao antibody-drug conjugates (ADCs), peptide-drug conjugates, me etahi atu 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
Ko tenei pūhui he parenga, he lysine derivative kua whakamahia i roto i te whakahiato peptide me te whanaketanga conjugate tarukino. Kei roto i te roopu Fmoc mo te whakamarumaru N-terminal, me te whakarereke-taha me te Eic(OtBu) (waikawa heicosanoic derivative), waikawa γ-glutamic (γ-Glu), me te AEEA (aminoethoxyethoxyacetate). I hangaia enei waahanga ki te ako i nga paanga lipidation, te matū mokowhiti, me te tuku raau taero. Kei te rangahau whanui i roto i te horopaki o nga rautaki prodrug, hononga ADC, me nga peptides tauwhitiwhiti 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
He pärönaki lysine kua whakarerekëtia te pühui nei e whakamahia ana i roto i te whakahiato peptide, ina koa mo te hanga i nga hononga peptide i whäia, maha-maha ranei. Ka taea e te roopu Fmoc te whakahiato hikoi ma te Fmoc toka-waahanga peptide synthesis (SPPS). Ka whakarereketia te mekameka taha ki te waikawa stearic waikawa (Ste), te waikawa γ-glutamic (γ-Glu), me nga hononga AEEA e rua (aminoethoxyethoxyacetate), e whakarato ana i te hydrophobicity, nga taonga utu, me te mokowhiti ngawari. Kei te rangahauhia mo tana mahi i roto i nga punaha tuku tarukino, tae atu ki nga antibody-drug conjugates (ADCs) me nga peptides-roto-a-roto.
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Boc-Tana(Trt)-Aib-Gln(Trt)-Gly-OH
Boc-Tana(Trt)-Aib-Gln(Trt)-Gly-OHhe tetrapeptide parea e whakamahia ana i roto i te whakahiato peptide me nga rangahau hanganga. Ko te roopu Boc (tert-butyloxycarbonyl) e tiaki ana i te N-terminus, ko nga roopu Trt (trityl) te tiaki i nga mekameka taha o te histidine me te glutamine hei aukati i nga tauhohenga kore. Ko te aroaro o Aib (a-aminoisobutyric acid) e whakatairanga ana i nga hanganga helical me te whakanui i te pumau o te peptide. He mea nui tenei peptide mo te tirotiro i te whakakopa peptide, te whakapumautanga, me te waahi mo te hoahoa peptides hohe koiora.
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Boc-Tyr(tBu)-Aib-Glu(OtBu)-Gly-OH
Boc-Tyr(tBu)-Aib-Glu(OtBu)-Gly-OHhe tetrapeptide parea e whakamahia ana i roto i te rangahau whakahiato peptide. Ko nga roopu Boc (tert-butyloxycarbonyl) me te tBu (tert-butyl) he roopu whakamarumaru hei aukati i nga tauhohenga taha i te wa o te huihuinga mekameka peptide. Ko te whakauru o te Aib (a-aminoisobutyric acid) ka awhina i nga hanganga helical me te whakanui ake i te pumau o te peptide. Ko tenei raupapa peptide e akohia ana mo tona kaha ki te wetewete ritenga, te whakakopa i te peptide, me te hei poraka whare ki te whakawhanake i nga peptides koiora me te pai ake o te pumau me te motuhake.
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Fmoc-Ile-Aib-OH
Ko te Fmoc-Ile-Aib-OH he poraka hanga dipeptide e whakamahia ana i roto i te whakahiato peptide-waahanga (SPPS). Ka honohia e ia te isoleucine e tiakina ana e Fmoc me te Aib (a-aminoisobutyric acid), he waikawa amino kore-taiao e whakarei ake ana i te pumau o te helix me te aukati 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
Ko te Fmoc-L-Lys[Eic(OtBu)-γ-Glu(OtBu)-AEEA-AEEA]-OH he paraka hanga waikawa amino i hangaia mo te tuku tarukino me te bioconjugation. Kei roto i te waahanga Eic (eicosanoid) mo te taunekeneke lipid, γ-Glu mo te whaainga, me nga mokowhiti AEEA mo te ngawari.
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Boc-Tyr(tBu)-Aib-OH
Ko te Boc-Tyr(tBu)-Aib-OH he poraka hangahanga dipeptide whakamarumaru e whakamahia ana i roto i te whakahiato peptide, te whakakotahi i te tyrosine kua tiakina e Boc me te Aib (a-aminoisobutyric acid). Ko te toenga o te Aib ka whakarei ake i te hanga helix me te aukati protease.
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Boc-Tana(Trt)-Ala-Glu(OtBu)-Gly-OH
Ko Boc-His(Trt)-Ala-Glu(OtBu)-Gly-OH he kongakonga tetrapeptide parea e whakamahia ana i roto i te whakahiato peptide-waahanga totoka (SPPS) me te whanaketanga tarukino peptide. Kei roto ko nga roopu whakamarumaru mo te whakahiato orthogonal me te whakaatu i tetahi raupapa whai hua ki te hoahoa peptide koiora me te hanganga.