Ngwa nri ọgwụ
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sodium na-ebelata
Inclisiran sodium API (Active Pharmaceutical Ingredient) ka a na-amụ nke ọma na nnyonye anya RNA (RNAi) na ọgwụgwọ ọrịa obi. Dị ka siRNA nwere eriri okpukpu abụọ na-ezubere iche maka mkpụrụ ndụ PCSK9, a na-eji ya na nyocha izizi yana nyocha ụlọ ọgwụ iji nyochaa usoro ịgbachi nkịtị na-eme ogologo oge maka iweda LDL-C (cholesterol lipoprotein dị ala). Ọ na-arụkwa ọrụ dị ka onyinye ihe atụ maka nyocha sistemu nnyefe siRNA, nkwụsi ike, yana ọgwụgwọ RNA lekwasịrị anya imeju.
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Fmoc-Gly-Gly-OH
Fmoc-Gly-Gly-OH bụ dipeptide a na-eji dị ka ihe mgbochi ụlọ n'ime peptide synthesis siri ike (SPPS). Ọ nwere ihe fọdụrụ glycine abụọ yana N-terminus na-echebe Fmoc, na-enye ohere maka elongation peptide chain nke na-achịkwa. N'ihi obere nha na mgbanwe nke glycine, a na-amụkarị dipeptide a n'ihe gbasara ọkpụkpụ azụ azụ peptide, nhazi njikọ, na nhazi nhazi na peptides na protein.
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Fmoc-Thr(tBu) -Phe-OH
Fmoc-Thr (tBu) -Phe-OH bụ ngọngọ ụlọ dipeptide nke a na-ejikarị na njikọ peptide siri ike (SPPS). Otu Fmoc (9-fluorenylmethyloxycarbonyl) na-echebe N-terminus, ebe otu tBu (tert-butyl) na-echebe ụdọ akụkụ hydroxyl nke threonine. A na-amụ dipeptide a echedoro maka ọrụ ya n'ịkwado elongation peptide nke ọma, na-ebelata ịgba ọsọ, na ịdepụta ebumnuche usoro kpọmkwem na nhazi protein na ọmụmụ mmekọrịta.
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AEEA-AEEA
AEEA-AEEA bụ hydrophilic, spacer na-agbanwe agbanwe nke a na-ejikarị na nyocha peptide na njikọ ọgwụ. Ọ mejupụtara nkeji abụọ ethylene glycol, na-eme ka ọ baa uru maka ịmụ ihe mmetụta nke ogologo njikọ na mgbanwe na mmekọrịta molecular, solubility, na ọrụ ndu. Ndị na-eme nchọpụta na-ejikarị nkeji AEEA nyochaa ka ndị na-ahụ maka oghere si emetụta arụmọrụ nke antibody-drug conjugates (ADCs), conjugates peptide-drug conjugates, na ndị ọzọ 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
Ngwakọta a bụ ihe eji emepụta lysine na-echebe, arụ ọrụ nke ejiri mee ihe na njikọ peptide na mmepe conjugate ọgwụ. Ọ na-egosipụta otu Fmoc maka nchebe N-ọnụ, yana mgbanwe n'akụkụ ya na Eic (OtBu) (eicosanoic acid derivative), γ-glutamic acid (γ-Glu), na AEEA (aminoethoxyethoxyacetate). Emebere ihe ndị a iji mụọ mmetụta lipidation, kemistri spacer, na mwepụta ọgwụ a na-achịkwa. A na-enyocha ya nke ọma n'ihe gbasara atụmatụ prodrug, ADC linkers na peptides na-emekọrịta ihe.
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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
Ngwakọta a bụ ihe lysine emezigharịrị eji eme ihe na njikọ peptide, ọkachasị maka imepụta conjugates peptide ezubere iche ma ọ bụ multifunctional. Otu Fmoc na-enye ohere maka njikọ nzọụkwụ site na Fmoc solid-phase peptide synthesis (SPPS). A na-eji ihe nrụpụta stearic acid (Ste), γ-glutamic acid (γ-Glu), na njikọ AEEA abụọ (aminoethoxyethoxyethoxyacetate), nke na-enye hydrophobicity, njikwa ụgwọ, na oghere mgbanwe. A na-amụkarị ya maka ọrụ ya na sistemụ nnyefe ọgwụ, gụnyere antibody-drug conjugates (ADCs) na peptides na-abanye cell.
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Boc-His(Trt)-Aib-Gln(Trt)-Gly-OH
Boc-His(Trt)-Aib-Gln(Trt)-Gly-OHbụ tetrapeptide echedoro nke ejiri na njikọ peptide na ọmụmụ ihe nhazi. Otu Boc (tert-butyloxycarbonyl) na-echebe N-terminus, ebe ndị otu Trt (tryl) na-echebe ụdọ akụkụ nke histidine na glutamine iji gbochie mmeghachi omume na-achọghị. Ọnụnọ nke Aib (α-aminoisobutyric acid) na-akwalite nhazi nke helical ma na-eme ka nkwụsi ike peptide dịkwuo elu. Ihe peptide a bara uru maka nyocha mpịakọta peptide, nkwụsi ike, yana dịka ihe nhụcha maka imepụta peptides na-arụ ọrụ ndụ.
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Boc-Tyr(tBu)-Aib-Glu(OtBu)-Gly-OH
Boc-Tyr(tBu)-Aib-Glu(OtBu)-Gly-OHbụ tetrapeptide echedoro nke a na-ejikarị na nyocha njikọ peptide. Otu Boc (tert-butyloxycarbonyl) na tBu (tert-butyl) na-eje ozi dị ka otu nchekwa iji gbochie mmeghachi omume akụkụ n'oge mgbakọ peptide chain. Ntinye nke Aib (α-aminoisobutyric acid) na-enyere aka ime ka ihe owuwu helical na-abawanye nkwụsi ike peptide. A na-amụ usoro peptide a maka ike ọ nwere na nyocha nhazi, mpịakọta peptide, yana dịka ihe mgbochi ụlọ n'ịzụlite peptides bioactive nwere nkwụsi ike na nkọwapụta.
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Fmoc-Ile-Aib-OH
Fmoc-Ile-Aib-OH bụ ngọngọ ụlọ dipeptide ejiri mee ihe na njikọ peptide siri ike (SPPS). Ọ na-ejikọta Fmoc-protected isoleucine na Aib (α-aminoisobutyric acid), amino acid na-abụghị eke nke na-eme ka nkwụsi ike helix na nkwụsị 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 bụ ngọngọ ụlọ amino acid arụrụ arụ ọrụ emebere maka nnyefe ọgwụ ezubere iche na bioconjugation. Ọ na-egosipụta moiety Eic (eicosanoid) maka mmekọrịta egbugbere ọnụ, γ-Glu maka ebumnuche, yana AEEA spacers maka mgbanwe.
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Boc-Tyr(tBu) -Aib-OH
Boc-Tyr (tBu) -Aib-OH bụ ngọngọ ụlọ dipeptide na-echebe nke a na-eji na peptide synthesis, na-ejikọta Boc-echebe tyrosine na Aib (α-aminoisobutyric acid). Ihe fọdụrụ nke Aib na-akwalite nhazi helix na nguzogide protease.
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Boc-His(Trt)-Ala-Glu(OtBu)-Gly-OH
Boc-His (Trt) -Ala-Glu (OtBu) - Gly-OH bụ mpempe tetrapeptide na-echebe nke a na-eji na-arụ ọrụ peptide siri ike (SPPS) na mmepe ọgwụ peptide. Ọ na-agụnye otu nchebe maka njikọ orthogonal ma nwee usoro bara uru na nhazi peptide bioactive na nhazi.