I-Cagrilintide iyi-analog ye-amylin esebenza isikhathi eside. Amylin iyi-hormone ye-peptide ekhiqizwa ngokuhlanganyela ama-β-cell we-pancreatic ngokumelene ne-insulin; ukulawula ibhalansi yamandla ngokusutha, ukubambezeleka kokukhipha isisu, kanye nokuvimbela i-glucagon.
I-amylin eyenzeka ngokwemvelo, ihlanganisa kalula futhi inozinzo oluphansi, ukunciphisa ukusetshenziswa kwabo emtholampilo. Ama-analogue asuselwa ku-amylin asekuqaleni afana i-pramlintide idinga imijovo ejwayelekile ngenxa ye-pharmacokinetics enganele yemiphumela yokwelapha ngohlobo 2 isifo sikashukela.
I-Cagrilintide ifinyelela lesi senzo eside ngokuguqulwa kweketango le-fatty acid eyingqayizivele – kanye i-dosing yamasonto onke iyindawo yokugcina efunwayo. Izivivinyo zemitholampilo zibonise imiphumela enamandla yokucindezela ukudla, indlela ehambisanayo yokusebenza eboniswayo uma iqhathaniswa ne-semaglutide.
Inhlanganisela yesilinganiso esingaguquki (I-CagriSema) ithuthukisiwe. Idatha yokuhlola yokunciphisa isisindo ibonisa ukuthi inhlanganisela idlula noma iyiphi i-ejenti iyodwa ngokusebenza ngempumelelo.
Ukuthuthuka okuqhubekayo kwe-cagrilintide kwandisa amandla okwelapha achazwe ngaphambilini we-amylin mimetics.; Ukwelashwa kwe-synergistic okuhlosiwe okuningi kokuphazamiseka kwe-metabolic kuyisiqondiso esicacile esizayo.
Ukulandelana
{I-Eicsanedioic acid-γ-Glu}-Lys-Cys-Asn-Thr-Ala-Thr-Cys-Ala-Thr-Gln-Arg-Leu-Ala-Glu-Phe-Leu-Arg-His-Ser-Asn-Asn-Phe-Gly-Pro-Ile-Leu-Pro-Thr-Asn-Val-Val-Asn-Ser- (Ibhuloho le-Disulfide:I-Cys3-Cys8)
Inombolo ye-CAS
1415456-99-3
I-Molecular Formula
I-C194H312N54O59S2
Isisindo samangqamuzana
4409.01 g/mol
Ucwaningo Oluhlobene Ne-Cagrilintide
1.Ukunciphisa Isifiso Sokudla kanye Nokuthuthukisa Ukusutha
Njenge-analog ye-amylin, ukuwela ngokushesha kwesithiyo sobuchopho begazi kuyisihluthulelo somphumela weCagrilintide.
Ukuqondiswa okuqondile kwezifunda ezithile zobuchopho ezilawula 'indlala’ yikho okuhlukanisayo – ukusebenza kwe i-calcitonin receptor (ukusayina kokwanela kwamandla) kunciphisa, uma kungenjalo aqeda, izifiso zokudla emaphakathi.
Ukudla okusekelwe ekuzimiseleni akukwazi ukuphindaphinda lolu shintsho lomzimba endaweni ebekiwe yomuntu.
2.Ukubambezeleka ekukhishweni kwesisu kanye nakho konke ukugaya okulandelayo
Ukuvinjelwa kokufinyela kwemisipha yesisu esibushelelezi kanye nokuphumuza kancane kwe-pylorus kunikeza uhlobo olungokwenyama oluqhubekayo lokugcwala okuqhubekayo..
Ukumuncwa kwezakhi kuyancishiswa, i-postprandial blood glucose (futhi ngokwezinga elikhulu yonke imingcele ye-metabolic) zigcinwa zizinzile ngangokunokwenzeka.
3.Ivimbela ukukhiqizwa kweglucagon ye-postprandial
I-Glucagon iyi-hormone ekhuthaza isibindi i-glycogenolysis futhi i-gluconeogenesis; ukusebenza ngempumelelo njenge-a i-ejenti ye-hyperglycemic.
I-Cagrilintide ilingisa imfihlo ye-postprandial ethize kakhulu amaseli alpha yenza, ukukhombisa ngesistimu yezinzwa zobuchopho ukuthi lokhu kukhululwa kwenzeke.
Ukwehliswa okukhulu ekukhiqizweni okukhulunywe ngakho kuwumphumela wokugcina – ukwehlisa ushukela wegazi we-postprandial kube enye yezinzuzo eziyinhloko.
Ukuthuthukisa amaphethini okudla ohlobo 2 iziguli ezinesifo sikashukela zisondelene kakhulu nale nqubo; zisebenzisa izinhlobo ezihlukahlukene ‘zamandla’ ingasondelwa ngokuzethemba okuphelele ngaphandle kokuqapha njalo kwe-glucose.
4.Isenzo se-Synergistic nge I-GLP-1 Receptor Agonists
Kuboniswa izindlela ezihambisana kakhulu phakathi kwe-cagrilintide nalawa ma-agonists.
I-GLP-1 ngokwayo igxile kakhulu ekusutheni, ngenkathi i-amylin analogues (ngokwezinga eliseduze eliphelele) cindezela zonke izinhlobo zendlala.
Indlela ekabili, okuhloswe ngakho okuningi i-pathophysiology indlela esekelwe ukukhuluphala kanye nesifo sikashukela yilokho inhlanganisela inikeza.
Izifundo (I-CagriSema eyakamuva kakhulu) baye babonisa ukwehla kwesisindo esiphakeme kanye nokulawulwa okuthuthukisiwe kwe-glycemic lapho kokubili kusetshenziswa ndawonye.
I-COA
I-HPLC
MS
