Magungunan Magunguna

Ciwon sodium

Inclisiran sodium API (Active Pharmaceutical Ingredient) ana nazarinsa da farko a fagen tsoma bakin RNA (RNAi) da kuma hanyoyin kwantar da hankali na zuciya. A matsayin siRNA mai madauri biyu da ke niyya ga kwayar PCSK9, ana amfani da shi a cikin bincike na gaskiya da na asibiti don kimanta dabarun yin shiru na dogon aiki don rage LDL-C (cholesterol mai ƙarancin yawa). Hakanan yana aiki azaman abin ƙira don bincika tsarin isar da siRNA, kwanciyar hankali, da magungunan RNA mai niyya da hanta.

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Fmoc-Gly-Gly-OH

Fmoc-Gly-Gly-OH dipeptide ne da aka yi amfani da shi azaman tushen ginin gini a cikin haɗakar peptide mai ƙarfi (SPPS). Yana fasalta ragowar glycine guda biyu da kuma N-terminus mai kariya ta Fmoc, yana ba da izinin haɓaka sarkar peptide mai sarrafawa. Saboda ƙananan girman glycine da sassauci, ana yin nazarin wannan dipeptide sau da yawa a cikin mahallin motsin kashin baya na peptide, ƙirar haɗin gwiwa, da ƙirar ƙirar tsari a cikin peptides da sunadarai.

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Fmoc-Thr(tBu) -Phe-OH

Fmoc-Thr(tBu) -Phe-OH tubalin ginin dipeptide ne wanda aka saba amfani dashi a cikin hadadden peptide synthesis (SPPS). Ƙungiyar Fmoc (9-fluorenylmethyloxycarbonyl) tana kare N-terminus, yayin da ƙungiyar tBu (tert-butyl) ke kare sarkar gefen hydroxyl na threonine. Ana nazarin wannan kariya ta dipeptide don rawar da yake takawa wajen sauƙaƙe haɓakar haɓakar peptide mai inganci, rage tseren tsere, da ƙirar ƙayyadaddun ƙayyadaddun jigogi a cikin tsarin furotin da nazarin hulɗa.

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AEEA-AEEA

AEEA-AEEA hydrophilic ne, mai sassauƙan sararin samaniya wanda aka saba amfani dashi a cikin binciken peptide da haɗin gwiwar ƙwayoyi. Ya ƙunshi raka'a biyu na tushen ethylene glycol, yana mai da amfani don nazarin tasirin haɗin haɗin gwiwa da sassauci akan hulɗar kwayoyin halitta, solubility, da ayyukan nazarin halittu. Masu bincike sukan yi amfani da sassan AEEA don tantance yadda masu sararin samaniya ke yin tasiri ga ayyukan haɗin gwiwar magungunan antibody-drug (ADCs), peptide-drog conjugates, da sauran bioconjugates.

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Fmoc-L-Lys[Eic(OtBu)-γ-Glu(OtBu)-AEEA]-OH

Wannan fili shine kariyar lysine mai aiki, wanda aka yi amfani da shi a cikin haɗin peptide da haɓaka haɗin magunguna. Yana fasalta ƙungiyar Fmoc don kariyar N-terminal, da gyare-gyare na gefe tare da Eic (OtBu) (eicosanoic acid derivative), γ-glutamic acid (γ-Glu), da AEEA (aminoethoxyethoxyacetate). An ƙera waɗannan abubuwan haɗin gwiwa don nazarin tasirin lipidation, sinadarai ta sarari, da sakin magunguna masu sarrafawa. An yi bincike sosai a cikin mahallin dabarun samar da magunguna, masu haɗin ADC, da peptides masu mu'amala da membrane.

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Fmoc-L-Lys[Ste(OtBu)-γ-Glu-(OtBu)-AEEA-AEEA]-OH

Wannan fili wani nau'in lysine ne da aka gyara wanda aka yi amfani da shi a cikin haɗin peptide, musamman don gina haɗin gwiwar peptide da aka yi niyya ko multifunctional. Ƙungiyar Fmoc tana ba da damar yin kira ta hanyar mataki ta hanyar Fmoc solid-phase peptide synthesis (SPPS). An gyaggyara sarkar gefen tare da stearic acid wanda aka samu (Ste), γ-glutamic acid (γ-Glu), da masu haɗin AEEA guda biyu (aminoethoxyethoxyethoxyacetate), waɗanda ke ba da hydrophobicity, kaddarorin caji, da tazara mai sassauƙa. Ana yawan nazarin shi don rawar da yake takawa a cikin tsarin isar da magunguna, gami da haɗin gwiwar magungunan rigakafi (ADCs) da peptides masu shiga tantanin halitta.

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Boc-His(Trt)-Aib-Gln(Trt)-Gly-OH

Boc-His(Trt)-Aib-Gln(Trt)-Gly-OHwani tetrapeptide mai kariya ne da ake amfani dashi a cikin haɗin peptide da nazarin tsarin. Ƙungiyar Boc (tert-butyloxycarbonyl) tana kare N-terminus, yayin da ƙungiyoyin Trt (tryl) ke kare sassan sassan histidine da glutamine don hana halayen da ba a so. Kasancewar Aib (α-aminoisobutyric acid) yana haɓaka haɓakar haɓakar helical kuma yana haɓaka kwanciyar hankali na peptide. Wannan peptide yana da kima don bincikar nadawa peptide, kwanciyar hankali, da kuma a matsayin siffa don zayyana peptides masu aiki da ilimin halitta.

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Boc-Tyr(tBu)-Aib-Glu(OtBu) -Gly-OH

Boc-Tyr(tBu)-Aib-Glu(OtBu) -Gly-OHwani tetrapeptide ne mai kariya wanda aka saba amfani dashi a cikin binciken haɗin peptide. Ƙungiyoyin Boc (tert-butyloxycarbonyl) da tBu (tert-butyl) suna zama ƙungiyoyi masu kariya don hana halayen gefe yayin taron sarkar peptide. Haɗin Aib (α-aminoisobutyric acid) yana taimakawa wajen haifar da sifofin helical da haɓaka kwanciyar hankali na peptide. Ana nazarin wannan jeri na peptide don yuwuwar sa a cikin bincike mai daidaituwa, nadewa peptide, da kuma matsayin tubalin gini don haɓaka peptides na bioactive tare da ingantaccen kwanciyar hankali da ƙayyadaddun bayanai.

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Fmoc-Ile-Aib-OH

Fmoc-Ile-Aib-OH tubalin ginin dipeptide ne da ake amfani da shi a cikin haɗakar peptide mai ƙarfi (SPPS). Ya haɗu da isoleucine mai kariya na Fmoc tare da Aib (α-aminoisobutyric acid), amino acid wanda ba na halitta ba wanda ke haɓaka kwanciyar hankali na helix da juriya na protease.

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Fmoc-L-Lys[Eic(OtBu)-γ-Glu(OtBu)-AEEA-AEEA]-OH

Fmoc-L-Lys [Eic(OtBu)-γ-Glu(OtBu) -AEEA-AEEA] -OH tubalin ginin amino acid ne mai aiki wanda aka ƙera don isar da magunguna da aka yi niyya da haɓakar halittu. Yana fasalta nau'in Eic (eicosanoid) don hulɗar lipid, γ-Glu don niyya, da AEEA sarari don sassauci.

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Boc-Tyr (tBu) - Aib-OH

Boc-Tyr (tBu) -Aib-OH wani shingen ginin dipeptide mai kariya wanda aka yi amfani dashi a cikin haɗin peptide, yana haɗa Boc-protected tyrosine da Aib (α-aminoisobutyric acid). Ragowar Aib yana haɓaka samuwar helix da juriya na protease.

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Boc-His(Trt)-Ala-Glu(OtBu)-Gly-OH

Boc-His (Trt) -Ala-Glu (OtBu) - Gly-OH wani yanki ne mai kariya na tetrapeptide wanda aka yi amfani da shi a cikin haɓakar peptide mai ƙarfi (SPPS) da ci gaban peptide miyagun ƙwayoyi. Ya haɗa da ƙungiyoyin karewa don haɗakarwa ta orthogonal kuma yana fasalta jeri mai amfani a ƙirar bioactive da tsarin peptide.

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