Zosakaniza za Pharma
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Kuphatikizika kwa sodium
Inclisiran sodium API (Active Pharmaceutical Ingredient) imaphunziridwa makamaka m'munda wa RNA interference (RNAi) ndi mankhwala a mtima. Monga siRNA yokhala ndi mizere iwiri yolunjika ku jini ya PCSK9, imagwiritsidwa ntchito pofufuza zachipatala komanso zachipatala kuti awunike njira zochepetsera jini zochepetsera LDL-C (low-density lipoprotein cholesterol). Imagwiranso ntchito ngati gawo lachitsanzo pakufufuza njira zoperekera siRNA, kukhazikika, komanso njira zochizira za RNA zomwe zimayang'aniridwa ndi chiwindi.
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Fmoc-Gly-Gly-OH
Fmoc-Gly-Gly-OH ndi dipeptide yomwe imagwiritsidwa ntchito ngati maziko omangira mu solid-phase peptide synthesis (SPPS). Imakhala ndi zotsalira ziwiri za glycine ndi Fmoc-protected N-terminus, zomwe zimalola kuti peptide chain italike. Chifukwa chakuchepa kwa glycine komanso kusinthasintha kwake, dipeptide iyi nthawi zambiri imawerengedwa potengera kusinthika kwa msana wa peptide, kapangidwe ka maulalo, komanso kutengera mawonekedwe a peptide ndi mapuloteni.
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Fmoc-Thr(tBu)-Phe-OH
Fmoc-Thr(tBu)-Phe-OH ndi chomangira cha dipeptide chomwe chimagwiritsidwa ntchito kwambiri popanga peptide synthesis (SPPS). Gulu la Fmoc (9-fluorenylmethyloxycarbonyl) limateteza N-terminus, pamene gulu la tBu (tert-butyl) limateteza mbali ya hydroxyl ya threonine. dipeptide yotetezedwayi imaphunziridwa chifukwa cha gawo lake pothandizira kuti peptide italikidwe bwino, kuchepetsa kuthamanga kwamtundu, komanso kutengera mitundu yotsatizana pamapangidwe a mapuloteni ndi maphunziro oyanjana.
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AEEA-AEEA
AEEA-AEEA ndi hydrophilic, flexible spacer yomwe imagwiritsidwa ntchito pofufuza peptide ndi mankhwala osokoneza bongo. Zili ndi mayunitsi awiri a ethylene glycol, zomwe zimapangitsa kuti zikhale zothandiza pophunzira zotsatira za kutalika kwa linker ndi kusinthasintha pa kuyanjana kwa maselo, kusungunuka, ndi zochitika zamoyo. Ofufuza nthawi zambiri amagwiritsa ntchito mayunitsi a AEEA kuti awunike momwe ma spacers amakhudzira magwiridwe antchito a antibody-drug conjugates (ADCs), peptide-drug conjugates, ndi ma bioconjugates ena.
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![Fmoc-L-Ls[Eic(OtBu)-γ-Glu(OtBu)-AEEA]-OH](https://cdn.globalso.com/gentolexgroup/Glepaglutide10-300x300.png)
Fmoc-L-Ls[Eic(OtBu)-γ-Glu(OtBu)-AEEA]-OH
Pawiri izi ndi otetezedwa, functionalized lysine zotumphukira ntchito peptide kaphatikizidwe ndi mankhwala conjugate chitukuko. Imakhala ndi gulu la Fmoc la chitetezo cha N-terminal, ndi kusintha kwa unyolo wam'mbali ndi Eic (OtBu) (eicosanoic acid derivative), γ-glutamic acid (γ-Glu), ndi AEEA (aminoethoxyethoxyacetate). Zidazi zidapangidwa kuti ziphunzire za lipidation, chemistry ya spacer, komanso kutulutsidwa kwa mankhwala olamulidwa. Amafufuzidwa kwambiri potengera njira za mankhwala, zolumikizira za ADC, ndi ma peptides olumikizana ndi membrane.
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![Fmoc-L-Ls[Ste(OtBu)-γ-Glu-(OtBu)-AEEA-AEEA]-OH](https://cdn.globalso.com/gentolexgroup/Glepaglutide9-300x300.png)
Fmoc-L-Ls[Ste(OtBu)-γ-Glu-(OtBu)-AEEA-AEEA]-OH
Chophatikizika ichi ndi chochokera ku lysine chosinthidwa chomwe chimagwiritsidwa ntchito popanga peptide, makamaka popanga ma conjugates olunjika kapena amitundu yambiri. Gulu la Fmoc limalola kuphatikizika kwapang'onopang'ono kudzera pa Fmoc solid-phase peptide synthesis (SPPS). Unyolo wam'mbali umasinthidwa ndi chochokera ku stearic acid (Ste), γ-glutamic acid (γ-Glu), ndi zolumikizira ziwiri za AEEA (aminoethoxyethoxyacetate), zomwe zimapereka hydrophobicity, katundu wacharge, komanso malo osinthika. Amaphunziridwa nthawi zambiri chifukwa cha gawo lake pamakina operekera mankhwala, kuphatikiza ma antibody-drug conjugates (ADCs) ndi ma peptides olowa m'maselo.
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Boc-His(Trt)-Aib-Gln(Trt)-Gly-OH
Boc-His(Trt)-Aib-Gln(Trt)-Gly-OHndi tetrapeptide yotetezedwa yomwe imagwiritsidwa ntchito popanga peptide ndi maphunziro apangidwe. Gulu la Boc (tert-butyloxycarbonyl) limateteza N-terminus, pamene magulu a Trt (trityl) amateteza unyolo wam'mbali wa histidine ndi glutamine kuti ateteze zochita zosafunikira. Kukhalapo kwa Aib (α-aminoisobutyric acid) kumalimbikitsa ma helical conformations ndikuwonjezera kukhazikika kwa peptide. Peptide iyi ndiyofunikira pakufufuza kupindika kwa ma peptide, kukhazikika, komanso ngati scaffold popanga ma peptide omwe amagwira ntchito mwachilengedwe.
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Boc-Tyr(tBu)-Aib-Glu(OtBu)-Gly-OH
Boc-Tyr(tBu)-Aib-Glu(OtBu)-Gly-OHndi tetrapeptide yotetezedwa yomwe imagwiritsidwa ntchito pofufuza kaphatikizidwe ka peptide. Magulu a Boc (tert-butyloxycarbonyl) ndi tBu (tert-butyl) amagwira ntchito ngati magulu otchinjiriza kuti asatengere mbali pakupanga ma peptide. Kuphatikizidwa kwa Aib (α-aminoisobutyric acid) kumathandizira kupanga mapangidwe a helical ndikuwonjezera kukhazikika kwa peptide. Kutsatizana kwa peptide kumeneku kumaphunziridwa chifukwa cha kuthekera kwake pakuwunika kogwirizana, kupindika kwa peptide, komanso ngati chomangira pakupanga ma peptide a bioactive ndi kukhazikika kokhazikika komanso kukhazikika.
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Fmoc-Ile-Aib-OH
Fmoc-Ile-Aib-OH ndi chomangira cha dipeptide chomwe chimagwiritsidwa ntchito popanga peptide synthesis (SPPS). Zimaphatikiza Fmoc-protected isoleucine ndi Aib (α-aminoisobutyric acid), amino acid omwe si achilengedwe omwe amachititsa kuti helix ikhale yolimba komanso kukana kwa protease.
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![Fmoc-L-Ls[Eic(OtBu)-γ-Glu(OtBu)-AEEA-AEEA]-OH](https://cdn.globalso.com/gentolexgroup/Glepaglutide6-300x300.png)
Fmoc-L-Ls[Eic(OtBu)-γ-Glu(OtBu)-AEEA-AEEA]-OH
Fmoc-L-Lys[Eic(OtBu)-γ-Glu(OtBu)-AEEA-AEEA]-OH ndi chipika chomangira cha amino acid chomwe chimapangidwa kuti chizigwiritsidwa ntchito popereka mankhwala ndi bioconjugation. Imakhala ndi gawo la Eic (eicosanoid) lolumikizana ndi lipid, γ-Glu polunjika, ndi ma spacers a AEEA kuti athe kusinthasintha.
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Boc-Tyr(tBu)-Aib-OH
Boc-Tyr(tBu)-Aib-OH ndi chomangira chotetezedwa cha dipeptide chomwe chimagwiritsidwa ntchito popanga peptide, kuphatikiza Boc-protected tyrosine ndi Aib (α-aminoisobutyric acid). Zotsalira za Aib zimakulitsa mapangidwe a helix ndi kukana kwa protease.
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Boc-His(Trt)-Ala-Glu(OtBu)-Gly-OH
Boc-His(Trt)-Ala-Glu(OtBu)-Gly-OH ndi chidutswa chotetezedwa cha tetrapeptide chomwe chimagwiritsidwa ntchito popanga peptide synthesis (SPPS) ndi chitukuko cha mankhwala a peptide. Zimaphatikizapo magulu otetezera a orthogonal synthesis ndipo imakhala ndi ndondomeko yothandiza pakupanga mapangidwe a peptide.