Semaglutide Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217 Isticmaalka cilmi-baarista kaliya
Semaglutide, oo lagu iibiyo magacyada astaantaOzempic,WegovyiyoRybelsus, waa ahdawooyinka ka hortagga sonkorowgaloo isticmaalo daawayntanooca 2aad ee xanuunka macaankaiyo sidadaawada ka hortagga buurnaantamuddo dheermaareynta miisaanka, waxaa soo saarayNovo Nordisksanadkii 2012-kii. Semaglutide waa aGLP-1 agonist receptor, taasoo la micno ah in ay ku ekaysiinayso ficilka aadanahakordhin glucagon-sida peptide-1(GLP-1), oo markaa sii kordhayainsulindheecaanka iyo kordhintasonkorta dhiigatuurista iyo hagaajintaxakamaynta glycemic.Dhibaatooyinka soo raaca waxaa ka mid ah lallabbo, matag, shuban, calool xanuun, iyo calool istaag. Bishii Disembar 2017, nooca la isku duro ee Ozempic waa la ansixiyay.Bishii Sebtembar 2019, nooc afka laga qaadan karo (Rybelsus) ayaa la oggolaaday, iyo Juun 2021, irbad heersare ah oo lagu iibiyo magaca sumadda Wegovy ee maaraynta miisaanka muddada-dheer ee dadka waaweyn waxaa ansixiyay MareykankaMaamulka Cuntada iyo Dawooyinka(FDA).Bishii Janaayo ee 2023, FDA waxay siisay Novo Nordisk ogolaansho si ay dib ugu eegto summada si ay u muujiso in Rybelsus afka ah loo isticmaali karodaaweynta safka koowaadloogu talagalay dadka waaweyn ee qaba nooca 2-aad ee xanuunka-macnaheedu waa dadka aan horay u qaadan dawo kale oo sonkorowga ah. Sannadka 2020, semaglutide wuxuu ahaa daawada 129-aad ee inta badan loo qoro gudaha Mareykanka, iyadoo in ka badan 4 milyan oo daawo loo qoray. La mid ah: Rybelsus, Ozempic, NN9535, OG217SC, Isticmaalka cilmi-baarista kaliya.
Waxqabadka Nafleyda
| Sharaxaada | Semaglutide (Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217), oo ah glucagon-like peptide 1 (GLP-1) muddo dheer shaqaynaysa, waa analog.GLP-1 receptoragonist oo awood u leh daaweynta nooca 2 diabetes mellitus (T2DM). |
| Bartilmaameedyada | GLP-1 receptor |
| In vitro | Semaglutide waxaa loo xushay sida ugu wanaagsan hal mar musharrax todobaadle ah.Semaglutide waxay leedahay laba beddel oo amino acid ah marka la barbar dhigo bini'aadamka GLP-1 (Aib8, Arg34) waxaana laga soo saaray lysine 26. GLP-1R affinity ee semaglutide (0.38 ± 0.06 nM) ayaa saddex laab hoos u dhacay marka loo eego liraglutide, halka affinity albumin waa la kordhiyaa. |
| In vivo | Nolosha nuska ah ee balaasmaha waa 46.1 h ee doofaarka yar-yar ee raacaya maamulka iv, iyo semaglutide waxay leedahay MRT 63.6 h ka dib qaadashada qiyaasta doofaarka-yar-yar. |
Protocol (laga bilaabo tixraac)
| Cilmi-baarista Unugga: | ● Khadadka gacanta:Unugyada BHK ● U-ururinta:0.01 pM - 0.1 μM ● Waqtiga soo galitaanka:3 h ● Habka:Qaybaha barafaysan ee unugyada BHK ee muujiya hGLP-1R iyo CRE firefly luciferase labadaba (clone FCW467-12A/KZ10-1) waa la dhalaalin, laba jeer ayaa lagu maydhaa PBS, waxaana lagu hakiyaa si sax ah.Unugyada waxaa lagu dahaadhay 96-ceel saxan oo ah 5000 unug/ Ceel mug dhan 50 μL.Isku-dhafka la tijaabinayo waxaa lagu qasi jiray bakhtiiye iyo 50 μL aliquot waxaa lagu wareejiyaa saxanka ka kooban unugyadu si loo gaaro qiyaasaha qiimeynta ugu dambeysa ee 1 × 10-14- 1 × 10-7M. Saxanka waxa lagu duray 3 saacadood 5% CO2heerkulka 37 ° C.Saxanka waxaa loo oggolaaday inuu ku istaago heerkulka qolka 15 daqiiqo ka hor inta aan lagu darin 100 μL ee steadylite iyo reagent.Saxanka waa la daboolay si looga ilaaliyo iftiinka waxaana lagu ruxayaa heerkulka qolka 30 daqiiqo.Saxanka waxa lagu akhriyaa aaladda TopCount NXT. |
Solubility (25°C)
| In vitroDufcaddii: | DMSO | 3 mg/ml(0.73 mm) |
| Ethanol | Aan la milmin | |
| Biyo | Aan la milmin |
Macluumaadka Kiimikada
| Miisaanka Molecular | 4113.58 | ||
| Formula | C187H291N45O59 | ||
| CAS Maya. | 910463-68-2 | ||
| Kaydinta | 3 sano | -20°C | budo |
| 2 sano | -80°C | dareere ku jira | |
| Rarida | Rarista heerkulka qolka(Walaac tayo leh oo bilaash ah: alaabtu waxay ku fiican tahay 37 ℃ ugu yaraan 1 toddobaad.) | ||
Macluumaadka Tijaabada Caafimaad
| Lambarka NCT | Shaqaalaysiinta | Faragelinta | Shuruudaha | Kafiil-qaatayaasha/Iskaashiga | Taariikhda billowga | Marxalada |
| NCT05537233 | Aan weli la qorin | Daawo: Semaglutide|Daawooyin: Placebo | Nooca 1 Sonkorowga|Cayilka | Jaamacadda Colorado Denver | Aasaaska Cilmi-baarista Sonkorowga Dhallaanka | Janaayo 1 2023 | Wajiga 2 |
| NCT04885634 | Aan weli la qorin | Daawo: Semaglutide Alaabta La Isku duro|Dawada: Placebo | Atrial Fibrillation|Miisaan xad dhaaf ah iyo cayil | Axel Brandes|Herlev iyo Gentofte Hospital|Hillerod Hospital Denmark |Svendborg Hospital | Oktoobar 2022 | Wajiga 3 |
| NCT05579977 | Shaqaalaysiinta | Daawooyinka: PF-07081532|Wax kale: Placebo|Daawoyinka: Rybelsus | Sonkorowga Mellitus|Cayilka | Pfizer | Oktoobar 27 2022 | Wajiga 2 |
| NCT05254314 | Shaqaalaysiinta | Dawooyinka: Semaglutide Qalinka Injector 2.4mg todobaadle | Mid kale: Placebo | Neefta | Xarunta Caafimaadka ee Jaamacadda Vanderbilt | Machadka Qaranka ee Xasaasiyadda iyo Cudurada Faafa (NIAID) | Sebtembar 7 2022 | Wajiga 2 |
| NCT05478252 | Shaqaalaysiinta | Daawo: Semaglutide J|Daawadii: Semaglutide B | Nooca 2aad ee Macaanka Mellitus | Novo Nordisk A/S | Ogosto 3 2022 | Wajiga 3 |
(xogta kahttps://clinicaltrials.gov, la cusbooneysiiyay 2022-11-29)
