Semaglutide Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217 No ka hoʻohana noiʻi wale nō
Semaglutide, kūʻai ʻia ma lalo o nā inoa inoaOzempic,ʻO WegovyaRybelsus, helāʻau antidiabetichoʻohana ʻia no ka mālama ʻana iʻano maʻi diabetes 2a e like melāʻau anti-obesityno ka wā lōʻihimālama kaumaha, hoʻomohala ʻia eNovo Nordiski ka makahiki 2012. ʻO Semaglutide kahiʻO GLP-1 agonist receptor, 'o ia ho'i, ho'ohālike ia i ka hana a ke kanakaincretin peptide-1 like me ka glucagon(GLP-1), ma laila e hoʻonui aiinsulinhuna a mahuahuakoko kokoka hoʻolei ʻana a me ka hoʻomaikaʻi ʻanahoʻomalu glycemic.ʻO nā hopena ʻaoʻao e pili ana i ka nausea, ka luaʻi, ka ʻōpū, ka ʻeha ʻōpū, a me ka constipation. I Dekemaba 2017, ua ʻae ʻia ka mana injectable i kapa ʻia ʻo Ozempic.I Kepakemapa 2019, ua ʻae ʻia kahi mana i hiki ke lawe ʻia e ka waha (Rybelsus), a ma Iune 2021, ua ʻae ʻia kahi injection kiʻekiʻe i kūʻai ʻia ma lalo o ka inoa inoa ʻo Wegovy no ka hoʻokele paona lōʻihi i nā pākeke i ʻae ʻia e ka USʻAi a me nā lāʻau lapaʻau(FDA).I Ianuali o 2023, hāʻawi ʻo FDA iā Novo Nordisk i ka ʻae e hoʻoponopono hou i ka lepili e hōʻike ai hiki ke hoʻohana ʻia ʻo Rybelsus waha ma ke ʻano helapaʻau muano ka poʻe mākua me ka maʻi maʻi ʻano 2—ʻo ia hoʻi i ka poʻe i lawe ʻole i ka lāʻau maʻi diabetes ma mua. I ka makahiki 2020, ʻo semaglutide ka 129th maʻamau i kuhikuhi ʻia i ka lāʻau lapaʻau ma ʻAmelika Hui Pū ʻIa, me ka ʻoi aku o 4 miliona mau lāʻau lapaʻau. Nā huaʻōlelo like: Rybelsus, Ozempic, NN9535, OG217SC, No ka hoʻohana noiʻi wale nō.
Hana Ola
| wehewehe | ʻO Semaglutide (Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217), he peptide like glucagon-like peptide 1 (GLP-1) lōʻihi, heʻO ka mea loaʻa GLP-1agonist me ka hiki ke mālama i ka maʻi diabetes type 2 (T2DM). |
| Nā pahu hopu | ʻO ka mea loaʻa GLP-1 |
| In vitro | Ua koho ʻia ʻo Semaglutide ma ke ʻano he koho maikaʻi loa i hoʻokahi pule pule.Loaʻa iā Semaglutide ʻelua mau mea hoʻololi amino acid i hoʻohālikelike ʻia me ke kanaka GLP-1 (Aib8, Arg34) a ua derivatized ma lysine 26. ʻO ka GLP-1R affinity o semaglutide (0.38 ± 0.06 nM) he ʻekolu mau manawa i hoʻohālikelike ʻia me ka liraglutide, ʻoiai ʻo ka albumin affinity. ua hoonuiia. |
| I loko o vivo | ʻO ka hapalua o ke ola o ka plasma he 46.1 mau hola ma nā puaʻa liʻiliʻi ma hope o ka hoʻokele iv, a he MRT ka semaglutide o 63.6 mau hola ma hope o ka sc dosing i nā puaʻa liʻiliʻi. |
Kūlana (mai ke kuhikuhi)
| Ke noiʻi pūnaewele: | ● Nā laina kelepona:BHK pūnaewele ● Kūlana:0.01 pM – 0.1 μM ● Manawa Incubation:3 h ● Hana:ʻO nā aliquots paʻa o nā pūnaewele BHK e hōʻike ana i ka hGLP-1R a me CRE firefly luciferase (clone FCW467-12A/KZ10-1) e hoʻoheheʻe ʻia, holoi ʻia ʻelua i ka PBS, a hoʻokuʻu ʻia i loko o ka assay buffer.Hoʻopili ʻia nā kelepona i loko o nā pā 96-well ma 5000 cell/well i ka nui o 50 μL.Hoʻoheheʻe ʻia nā pūhui e hoʻāʻo ʻia i loko o ka assay buffer a me kahi 50 μL aliquot i hoʻoili ʻia i ka pā i loaʻa nā cell e hiki ai i nā hoʻopaʻa hoʻāʻo hope loa o 1 × 10.−14− 1 × 10−7M. Hoʻokomo ʻia ka pā no 3 mau hola ma 5% CO2ma 37 °C.Ua ʻae ʻia ka pā e kū i ka lumi wela no 15 min ma mua o ka hoʻohui ʻana i 100 μL o ka steadylite me ka reagent.Ua uhi ʻia ka pā no ka pale ʻana mai ka mālamalama a hoʻoluliluli ʻia i ka lumi wela no 30 min.Heluhelu ʻia ka pā ma kahi mea hana TopCount NXT. |
Hoʻoheheʻe (25°C)
| In vitroPūʻulu: | DMSO | 3 mg/mL(0.73 mM) |
| Ethanol | ʻAʻole hiki ke hoʻoheheʻe | |
| Wai | ʻAʻole hiki ke hoʻoheheʻe |
ʻIkepili Kemika
| Kaumaha Molekala | 4113.58 | ||
| Kumukumu | C187H291N45O59 | ||
| CAS No. | 910463-68-2 | ||
| Waihona | 3 makahiki | -20°C | pauda |
| 2 makahiki | -80°C | i ka mea hoohehee | |
| Hoʻouna | Hoʻouna wela lumi(ʻAʻohe hopohopo maikaʻi: maikaʻi ka huahana ma 37 ℃ no ka liʻiliʻi o 1 pule.) | ||
ʻIkepili hoʻokolohua lapaʻau
| Helu NCT | Hoʻolimalima | Nā hoʻopaʻapaʻa | Nā kūlana | Kākoʻo/Kokua | lā hoʻomaka | Māhele |
| NCT05537233 | ʻAʻole i hoʻopaʻa inoa | Laau Laau: Semaglutide|Laau: Placebo | ʻAno maʻi maʻi maʻi 1|Obesity | Ke Kulanui o Colorado Denver|Juvenile Diabetes Research Foundation | Ianuali 1 2023 | Māhele 2 |
| NCT04885634 | ʻAʻole i hoʻopaʻa inoa | Laau Laau: Semaglutide Injectable Product|Laau: Placebo | Atrial Fibrillation|Ke kaumaha nui a me ka momona | Axel Brandes|Herlev and Gentofte Hospital|Hillerod Hospital Denmark|Svendborg Hospital|Hakapila o South West Jutland|Odense University Hospital | ʻOkakopa 2022 | Māhele 3 |
| NCT05579977 | Hoʻolimalima | Laau Laau: PF-07081532|E ae: Placebo|Laau Laau: Rybelsus | ʻO ka maʻi maʻi maʻi| | Pfizer | ʻOkakopa 27 2022 | Māhele 2 |
| NCT05254314 | Hoʻolimalima | Laau Laau: Semaglutide Pen Injector 2.4mg i kēlā me kēia pule|E aʻe: Placebo | Hānō | Vanderbilt University Medical Center|National Institute of Allergy and Infectious Diseases (NIAID) | Kepakemapa 7 2022 | Māhele 2 |
| NCT05478252 | Hoʻolimalima | Laau Laau: Semaglutide J|Laau Laau: Semaglutide B | ʻO ka maʻi diabetes type 2 | ʻO Novo Nordisk A/S | ʻAukake 3 2022 | Māhele 3 |
(ʻikepili maihttps://clinicaltrials.gov, hōʻano hou ʻia ma 2022-11-29)
