Semaglutide Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217 Mo suʻesuʻega faʻaaoga naʻo
Semaglutide, fa'atau atu i lalo o igoa fa'ailogaOzempic,WegovymaRybelsus, o sevaila'au fa'ama'i sukafa'aaogaina mo togafitiga oma'isuka ituaiga 2ma e pei ovaila'au fa'ama'i putamo se taimi umipuleaina o le mamafa, atiina ae eNovo Nordiski le 2012. Semaglutide o seGLP-1 receptor agonist, o lona uiga e fa'atusaina le gaioiga a le tagataincretin peptide e pei o le glucagon-1(GLP-1), o lea ua faateleina aiinisalinifa'alilo ma fa'ateleinatoto sukalafoai ma faaleleiapulea glycemic.O a'afiaga e aofia ai le faafaufau, pua'i, manava manava, tiga o le manava, ma le manava. I le masina o Tesema 2017, na faʻamaonia ai le injectable version e igoa ia Ozempic.Ia Setema 2019, na faʻamaonia ai se faʻamatalaga e mafai ona ave e le gutu (Rybelsus), ma ia Iuni 2021, o se tui maualuga maualuga na faʻatau atu i lalo o le igoa igoa Wegovy mo le puleaina o le mamafa umi i tagata matutua na faʻatagaina e le US.Pulega o Mea'ai ma Vailaau(FDA).Ia Ianuari o le 2023, na tuʻuina atu ai e le FDA le Novo Nordisk faʻatagaga e toe faʻaleleia le igoa e faʻaalia ai e mafai ona faʻaogaina le Rybelsus tautala e avea o setogafitiga muamuamo tagata matutua e maua i le ma'isuka ituaiga 2—o lona uiga i tagata e le'i inuina muamua se isi vaila'au o le ma'isuka. I le 2020, o le semaglutide o le 129th sili ona masani ona faʻatonuina vailaʻau i le Iunaite Setete, ma sili atu i le 4 miliona talavai. Synonyms: Rybelsus, Ozempic, NN9535, OG217SC, Mo na'o su'esu'ega fa'aoga.
Gaioiga Fa'aola
| Fa'amatalaga | Semaglutide (Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217), o se glucagon-pei o le peptide 1 (GLP-1) umi e galue, o seGLP-1 talitaliagonist e mafai ona togafitia le ma'isuka ituaiga 2 (T2DM). |
| Sini | GLP-1 talitali |
| In vitro | Semaglutide ua filifilia e avea ma sui sili ona lelei i vaiaso taʻitasi.Semaglutide e lua suiga amino acid pe a faʻatusatusa i le tagata GLP-1 (Aib8, Arg34) ma e maua mai i le lysine 26. O le GLP-1R affinity o semaglutide (0.38 ± 0.06 nM) e faʻatolu ona faʻaititia pe a faʻatusatusa i le liraglutide, ae o le albumin affinity. ua faateleina. |
| I vivo | Ole afa ole ola ole plasma ole 46.1 h ile tama'i pua'a pe a mae'a ile pulega iv, ma ole semaglutide o lo'o iai le MRT ole 63.6 h ina ua mae'a le tu'uina atu i pua'a laiti. |
Protocol (mai fa'asinomaga)
| Su'esu'ega sela: | ● Laina sela:BHK sela ● Fa'atonuga:0.01 pm – 0.1 μM ● Taimi Fa'a'au:3 h ● Metotia:Aliquots fa'aaisa o sela BHK o lo'o fa'aalia uma le hGLP-1R ma le CRE firefly luciferase (clone FCW467-12A/KZ10-1) o lo'o fa'afefeteina, fufulu fa'alua ile PBS, ma fa'agata ile su'ega su'ega.O sela o loʻo faʻapipiʻiina i fafo i totonu o le 96-well plates i le 5000 cell/well i se voluma o le 50 μL.O mea faʻafefiloi e faʻataʻitaʻiina o loʻo faʻafefeteina i le suʻega suʻega ma se 50 μL aliquot faʻafeiloaʻi i le ipu o loʻo i ai sela e oʻo atu i faʻamaʻi suʻesuʻega mulimuli o le 1 × 10−14− 1 × 10−7M. O lo'o fa'asusu le ipu mo le 3 itula ile 5% CO2i le 37 °C.O le ipu na faʻatagaina e tu i le vevela o le potu mo le 15 minute aʻo leʻi faʻaopoopoina le 100 μL o le steadylite faʻatasi ai ma le reagent.E ufiufi le ipu e puipuia mai le malamalama ma luluina i le vevela o le potu mo le 30 min.E faitau le ipu i se meafaigaluega TopCount NXT. |
Solu (25°C)
| In vitroVaega: | DMSO | 3 mg/mL(0.73 mM) |
| Ethanol | E le mafai ona fa'afefeteina | |
| Vai | E le mafai ona fa'afefeteina |
Fa'amatalaga vaila'au
| Molecular Weight | 4113.58 | ||
| Fuafuaga | C187H291N45O59 | ||
| CAS Nu. | 910463-68-2 | ||
| Teuina | 3 tausaga | -20°C | pauta |
| 2 tausaga | -80°C | i le solvent | |
| Va'a | La'uina o le vevela o le potu(E leai se popolega: o le oloa e lelei ile 37℃ mo le itiiti ifo ile 1 vaiaso.) | ||
Fa'amatalaga Fa'ata'ita'i Falema'i
| Numera NCT | Fa'afaigaluegaina | Fa'alavelave | Tulaga | Sponsor/Sponsors | Aso Amata | Vaega |
| NCT05537233 | E le'i fa'afaigaluegaina | Vailaau Fa'asaina: Semaglutide|Valaau: Placebo | Ituaiga 1 Ma'isuka|Obesa | Iunivesite o Colorado Denver|Juvenile Diabetes Research Foundation | Ianuari 1 2023 | Vaega 2 |
| NCT04885634 | E le'i fa'afaigaluegaina | Fualaau Fa'asaina: Semaglutide Injectable Product|Valaau: Placebo | Atrial Fibrillation|Ova Ova ma Opo | Axel Brandes|Herlev ma Gentofte Hospital|Hillerod Hospital Tenimaka|Svendborg Hospital|Hospital of South West Jutland|Odense University Hospital | Oketopa 2022 | Vaega 3 |
| NCT05579977 | Fa'afaigaluegaina | Vailaau Fa'asaina: PF-07081532|Isi: Placebo|Valaau: Rybelsus | Ma'isuka Mellitus|Obesa | Pfizer | Oketopa 27 2022 | Vaega 2 |
| NCT05254314 | Fa'afaigaluegaina | Vailaau Fa'asaina: Semaglutide Pen Injector 2.4mg i vaiaso ta'itasi|Isi: Placebo | Asma | Vanderbilt University Medical Center|National Institute of Allergy and Infectious Diseases (NIAID) | Setema 7 2022 | Vaega 2 |
| NCT05478252 | Fa'afaigaluegaina | Fualaau: Semaglutide J | Fualaau: Semaglutide B | Ma'isuka Mellitus Ituaiga 2 | Novo Nordisk A/S | Aokuso 3 2022 | Vaega 3 |
(faamatalaga maihttps://clinicaltrials.gov, fa'afou ile 2022-11-29)
