Semaglutide Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217 Mo te whakamahi rangahau anake
Semaglutide, hokona i raro i nga ingoa waitohuOzempic,WehiaRybelsus, herongoā antidiabeticwhakamahia mo te maimoatanga omate huka momo 2me te riterongoā anti-momonamo te wa roawhakahaere taimaha, i whakawhanakehia eNovo Nordiski te tau 2012. Ko te Semaglutide heGLP-1 agonist kaiwhakawhiwhi, te tikanga ka whakatauira i te mahi a te tangatawhakauru glucagon-rite peptide-1(GLP-1), ka piki akeinsulinte huna me te piki haerehuka totote tuku me te whakapai akete whakahaere glycemic.Ko nga paanga o te taha ko te nausea, te ruaki, te korere, te mamae o te puku, me te kookiri. I te Hakihea 2017, i whakaaetia te putanga injectable ko Ozempic.I te marama o Hepetema 2019, he putanga ka taea te tango ma te waha (Rybelsus) i whakaaetia, a i te Hune 2021, he werohanga nui ake i hokona i raro i te ingoa tohu Wegovy mo te whakahaere taumaha mo te wa roa i roto i nga pakeke i whakaaetia e te USWhakahaere Kai me te Taakaro(FDA).I te Hanuere o 2023, i tukuna e te FDA te whakaaetanga a Novo Nordisk ki te whakahou i te tapanga hei tohu ka taea te whakamahi a Rybelsus waha heimaimoatanga tuatahimo nga pakeke mate huka momo 2—te tikanga mo nga tangata kaore ano kia tango i tetahi atu rongoa mate huka. I te tau 2020, ko te semaglutide te 129 te nuinga o nga rongoa rongoa i Amerika, neke atu i te 4 miriona nga whakahaunga. Nga kupu taurite: Rybelsus, Ozempic, NN9535, OG217SC, Mo te whakamahi rangahau anake.
Mahi Koiora
Whakaahuatanga | Ko Semaglutide (Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217), he glucagon-like peptide 1 (GLP-1) he rite ki te roa o te mahi.GLP-1 kaiwhakawhiwhiagonist me te kaha mo te maimoatanga o te mate huka mellitus momo 2 (T2DM). |
Nga whainga | GLP-1 kaiwhakawhiwhi |
In vitro | Ka tohua a Semaglutide hei kaitono pai mo ia wiki.E rua nga whakakapinga waikawa amino a Semaglutide i whakaritea ki te GLP-1 tangata (Aib8, Arg34) ka whakahekehia i te lysine 26. Ko te hononga GLP-1R o semaglutide (0.38 ± 0.06 nM) e toru nga heke iho ki te liraglutide, engari ko te hononga o te albumin. kua piki ake. |
I roto i te vivo | Ko te haurua o te plasma he 46.1 h i roto i nga poaka iti i muri i te whakahaeretanga iv, a he MRT te semaglutide mo te 63.6 h i muri i te sc dosing ki nga poaka paku. |
Kawa (mai i te tohutoro)
Rangahau Pūtau: | ● Raina pūtau:BHK pūtau ● Ngā Kukū:0.01 pM – 0.1 μM ● Wā Heki:3 h ● Tikanga:Ko nga hautio tio o nga pūtau BHK e whakaatu ana i te hGLP-1R me te CRE firefly luciferase (clone FCW467-12A/KZ10-1) ka whakamarokehia, ka horoi rua ki te PBS, ka whakatarewahia ki roto i te parepare whakamatautau.Ka whakakikoruatia nga pūtau ki roto i nga pereti 96-puna i te 5000 pūtau/puna i roto i te rōrahi o te 50 μL.Ko nga puhui hei whakamatautau ka waimeha ki roto i te parepare whakamatautau me te 50 μL aliquot ka whakawhitia ki te pereti kei roto nga pūtau kia tae atu ki nga kohinga whakamatautau whakamutunga o te 1 × 10−14− 1 × 10−7M. Ka whakakororia te pereti mo te 3 haora i te 5% CO2i te 37 °C.I tukuna te pereti kia tu i te pāmahana rūma mo te 15 meneti i mua i te taapiri 100 μL o te steadylite me te reagent.Ka hipokina te pereti hei whakamarumaru mai i te marama ka ruia i te pāmahana rūma mo te 30 min.Ka panuihia te pereti ki tetahi taputapu TopCount NXT. |
Wairewa (25°C)
In vitropuranga: | DMSO | 3 mg/mL(0.73 mM) |
Ewaro | Korekore | |
Wai | Korekore |
Nga korero matū
Taumaha rāpoi | 4113.58 | ||
Tātai | C187H291N45O59 | ||
CAS No. | 910463-68-2 | ||
Rokiroki | 3 tau | -20°C | paura |
2 tau | -80°C | i te whakarewa | |
Te tuku | Te tuku i te pāmahana rūma(Karekau he awangawanga o te kounga: he pai te hua i te 37 ℃ mo te 1 wiki neke atu.) |
Nga korero mo te whakamatautau haumanu
Nama NCT | Te Rehita | Nga wawaotanga | Nga tikanga | Kaitautoko / Kaihoahoa | Rā Tīmata | Wāhanga |
NCT05537233 | Kaore ano kia kimihia | Taakaro: Semaglutide|Taukino: Placebo | Momo 1 mate huka|Momona | Te Whare Wananga o Colorado Denver|Juvenile Diabetes Research Foundation | Hanuere 1 2023 | Wāhanga 2 |
NCT04885634 | Kaore ano kia kimihia | Taakaro: Hua Injectable Semaglutide|Taukino: Placebo | Atrial Fibrillation|Te taumaha me te momona | Axel Brandes|Herlev and Gentofte Hospital|Hillerod Hospital Denmark|Svendborg Hospital|Hospital of South West Jutland|Odense University Hospital | Oketopa 2022 | Wāhanga 3 |
NCT05579977 | Te kimi mahi | Taakaro: PF-07081532|Tetahi atu: Placebo|Taukino: Rybelsus | Te mate huka|Momona | Pfizer | Oketopa 27 2022 | Wāhanga 2 |
NCT05254314 | Te kimi mahi | Ta'auau: Semaglutide Pene Injector 2.4mg ia wiki|Tetahi atu: Placebo | huangō | Vanderbilt University Medical Center|National Institute of Allergy and Infectious Diseases (NIAID) | Mahuru 7 2022 | Wāhanga 2 |
NCT05478252 | Te kimi mahi | Taakaro: Semaglutide J|Taukino: Semaglutide B | Te mate huka momo 2 | Novo Nordisk A/S | Akuhata 3 2022 | Wāhanga 3 |
(raraunga maihttps://clinicaltrials.gov, whakahōutia i te 2022-11-29)