Semaglutide Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217 Rau kev tshawb fawb siv nkaus xwb
Semaglutide, muag raws li cov npe khoom lag luamOzempic,WegovythiabRybelsus, yog ibtshuaj antidiabeticsiv rau kev kho mob ntawmmob ntshav qab zib hom 2thiab astshuaj tiv thaiv rograu lub sij hawm ntevtswj qhov hnyav, tsim los ntawmNovo Nordiskhauv 2012. Semaglutide yog ibGLP-1 receptor agonist, txhais tau tias nws ua raws li kev ua ntawm tib neegincretin glucagon zoo li peptide-1(GLP-1), yog li nceinsulinsecretion thiab ncentshav qab zibpov tseg thiab txhim khotswj glycemic.Cov kev mob tshwm sim muaj xws li xeev siab, ntuav, raws plab, mob plab, thiab cem quav. Thaum Lub Kaum Ob Hlis 2017, cov tshuaj txhaj tshuaj npe hu ua Ozempic tau pom zoo.Thaum lub Cuaj Hlis 2019, ib qho qauv uas tuaj yeem nqa los ntawm lub qhov ncauj (Rybelsus) tau pom zoo, thiab thaum Lub Rau Hli 2021, kev txhaj tshuaj ntau dua muag raws li lub npe Wegovy rau kev tswj qhov hnyav mus ntev hauv cov neeg laus tau pom zoo los ntawm AsmeskasFood and Drug Administration(FDA).Thaum Lub Ib Hlis Ntuj xyoo 2023, FDA tau tso cai rau Novo Nordisk los kho daim ntawv lo qhia tias qhov ncauj Rybelsus tuaj yeem siv los ua ib qhothawj kab kev kho mobrau cov neeg laus uas muaj ntshav qab zib hom 2 - txhais tau tias hauv cov neeg uas tsis tau noj lwm yam tshuaj ntshav qab zib. Xyoo 2020, semaglutide yog 129th feem ntau cov tshuaj kws kho mob hauv Tebchaws Meskas, nrog ntau dua 4 lab cov tshuaj. Synonyms: Rybelsus, Ozempic, NN9535, OG217SC, Rau kev tshawb fawb siv nkaus xwb.
Kev ua lom lom
| Kev piav qhia | Semaglutide (Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217), ib tug ntev-acting glucagon-zoo li peptide 1 (GLP-1) analogue,GLP-1 receptoragonist nrog lub peev xwm rau kev kho mob ntawm hom 2 mob ntshav qab zib mellitus (T2DM). |
| Hom phiaj | GLP-1 receptor |
| Hauv vitro | Semaglutide raug xaiv los ua qhov zoo tshaj plaws ib zaug tus neeg sib tw txhua lub lim tiam.Semaglutide muaj ob qhov kev hloov pauv amino acid piv rau tib neeg GLP-1 (Aib8, Arg34) thiab yog derivatized ntawm lysine 26. GLP-1R affinity ntawm semaglutide (0.38 ± 0.06 nM) yog peb-fold txo qis piv rau liraglutide, whereas lub albumin affinity yog nce. |
| Hauv vivo | Lub plasma ib nrab-lub neej yog 46.1 h hauv cov npua me me tom qab kev tswj hwm iv, thiab semaglutide muaj MRT ntawm 63.6 teev tom qab sc dosing rau cov npua me. |
Protocol (los ntawm kev siv)
| Kev tshawb fawb ntawm tes: | ● Cell kab:BHK hlwb ● Concentrations:0.01 pM - 0.1 μM ● Lub Sijhawm Incubation:3 h ua ● Txoj kev:Frozen aliquots ntawm BHK hlwb uas qhia ob qho tib si hGLP-1R thiab CRE firefly luciferase (clone FCW467-12A/KZ10-1) yog thawed, ntxuav ob zaug hauv PBS, thiab raug tshem tawm hauv kev soj ntsuam tsis.Cells yog plated tawm mus rau hauv 96-zoo daim hlau ntawm 5000 hlwb / zoo nyob rau hauv ib tug ntim ntawm 50 μL.Cov tshuaj uas yuav tsum tau kuaj yog diluted nyob rau hauv assay buffer thiab ib tug 50 μL aliquot pauv mus rau lub phaj uas muaj cov hlwb kom ncav cuag qhov kawg kev soj ntsuam concentration ntawm 1 × 10.—14- 1 × 10—7M. Lub phaj yog incubated rau 3 h ntawm 5% CO2ntawm 37 ° C.Lub phaj tau tso cai rau sawv ntsug ntawm chav sov li 15 feeb ua ntej ntxiv 100 μL ntawm steadylite ntxiv rau reagent.Lub phaj yog npog los tiv thaiv nws ntawm lub teeb thiab shaken ntawm chav tsev kub rau 30 min.Lub phaj tau nyeem hauv TopCount NXT ntsuas. |
Solubility (25 ° C)
| Hauv vitroBatch: | DMSO | 3 mg/ml(0.73 hli) |
| Ethanol | Insoluble | |
| Dej | Insoluble |
Cov ntaub ntawv tshuaj
| Molecular Luj | 4 113.58 | ||
| Formula | C187H291 ibN45O59 | ||
| CAS Nr. | 910463-68-2 | ||
| Cia | 3 xyoo | -20 ° C | hmoov |
| 2 xyoo | -80 ° C | hauv cov kuab tshuaj | |
| Shipping | Chav kub shipping(Kev txhawj xeeb tsis zoo: cov khoom zoo ntawm 37 ℃ tsawg kawg yog 1 lub lis piam.) | ||
Cov ntaub ntawv soj ntsuam kuaj mob
| NCT Num | Kev nrhiav neeg ua haujlwm | Kev cuam tshuam | Cov xwm txheej | Sponsor/Collaborators | Pib Hnub | Phase |
| NCT05537233 | Tseem tsis tau recruiting | Tshuaj: Semaglutide | Tshuaj: Placebo | Hom 1 Diabetes | Kev rog | Tsev kawm ntawv ntawm Colorado Denver | Cov Hluas Kev Tshawb Fawb Txog Kev Mob Ntshav Qab Zib | Lub Ib Hlis 1 2023 | Theem 2 |
| NCT04885634 | Tseem tsis tau recruiting | Tshuaj: Semaglutide Injectable Product | Tshuaj: Placebo | Atrial Fibrillation | Kev rog dhau thiab rog | Axel Brandes | Tsev Kho Mob Herlev thiab Gentofte | Tsev Kho Mob Hillerod Denmark | Tsev Kho Mob Svendborg | Tsev Kho Mob ntawm South West Jutland | Tsev Kho Mob Odense University | Lub Kaum Hli 2022 | Theem 3 |
| NCT05579977 | Kev nrhiav neeg ua haujlwm | Tshuaj: PF-07081532|Lwm Yam: Placebo|Drug: Rybelsus | Mob ntshav qab zib mellitus | Kev rog | Pfizer | Peb Hlis 27 2022 | Theem 2 |
| NCT05254314 | Kev nrhiav neeg ua haujlwm | Tshuaj: Semaglutide Pen Injector 2.4mg txhua lub lim tiam | Lwm yam: Placebo | Mob hawb pob | Vanderbilt University Medical Center|National Institute of Allergy and Infectious Diseases (NIAID) | Peb Hlis 7 2022 | Theem 2 |
| NCT05478252 | Kev nrhiav neeg ua haujlwm | Tshuaj: Semaglutide J | Tshuaj: Semaglutide B | Mob ntshav qab zib mellitus hom 2 | Novo Nordisk A/S | Aug 3 2022 | Theem 3 |
(cov ntaub ntawv los ntawmhttps://clinicaltrials.gov, tshiab 2022-11-29)
