Semaglutide(Rybelsus, Ozempic, NN9535, OG217SC, NNC0113-0217) yog ib qho ua haujlwm ntev glucagon-zoo li peptide-1 (GLP-1) analog thiab agonist ntawm GLP-1 receptor . Nws muaj peev xwm ua tau zoo hauv kev kho mob ntawm hom 2 mob ntshav qab zib mellitus (T2DM). Semaglutide yog tsim los ntawm cov qauv hauv paus ntawm liraglutide thiab tau pom tias muaj txiaj ntsig zoo hauv kev kho T2DM. Nws yog npaj siv cov khoom siv-theem synthesis, koom nrog cov khoom sib txuas ntawm cov kab peptide Aib8, Arg34GLP-1(7-37), thiab fatty acid side chain acylating agent. Nyob rau hauv alkaline tej yam kev mob, cov fatty acid sab saw acylating tus neeg saib xyuas yog siv los hloov cov ncaj-chain peptide Lys26, uas ua rau semaglutide. Cov qauv sib xyaw ua ke yog tom qab ntawd raug rau lub sijhawm daws teeb meem fluorescence resonance zog hloov immunoassay rau kev ntsuam xyuas bioactivity.
Piv rau liraglutide, semaglutide muaj cov roj fatty acid ntev dua, uas ua rau nws cov hydrophilicity nce. Txawm li cas los xij, semaglutide tau hloov kho nrog luv-chain polyethylene glycol (PEG), ua kom nws cov hydrophilicity. Kev hloov kho PEG tsis tsuas yog tso cai rau nws nruj nreem khi rau albumin, npog qhov chaw cleavage ntawm dipeptidyl peptidase-4 (DPP-4), tab sis kuj txo lub raum excretion, yog li ncua nws ib nrab-lub neej thiab ua tiav ntev. kev cuam tshuam.
Semaglutide yog tsim los ntawm Novo Nordisk thiab tau ua kom pom qhov zoo tshaj ntawm DPP {{{0}}} inhibitor sitagliptin thiab GLP ua haujlwm ntev -1 agonist exenatide (Bydureon) hauv kev sim tshuaj. Nws kuj tau muab piv rau lub taub hau-rau-lub taub hau nrog Lilly's Trulicity. Hauv kev sim, koob tshuaj semaglutide txo qis A1C qib los ntawm 1.6 feem pua thiab ua rau qhov hnyav tshaj plaws ntawm 6 kg. Kev ua tau zoo thiab kev nyab xeeb ntawm kev txhaj tshuaj ib zaug ib lim piam ntawm 1.0 mg semaglutide thiab 2.0 mg exenatide tau muab piv rau hauv 813 cov neeg mob ntshav qab zib hom 2 nyob rau lub sijhawm 56 lub lis piam. Cov neeg mob kuj tau txais ib mus rau ob qho tshuaj txo qis hauv qhov ncauj ib txhij. Thaum Lub Kaum Ob Hlis 2017, US FDA tau pom zoo Novo Nordisk's GLP ib lub lim tiam ib zaug -1 glucose-lowering tshuaj semaglutide, ua lag luam li Ozempic. Cov ntaub ntawv soj ntsuam kuaj pom tau tias Ozempic tuaj yeem txo HbA1c qib thiab muaj peev xwm pab cov neeg mob poob phaus, piv rau cov placebo, Merck's Januvia, AstraZeneca's Bydureon, thiab Sanofi's Lantus.
Raws li tus thawj coj hauv kev kho mob ntshav qab zib, Novo Nordisk tau tswj hwm GLP-1 kev ua lag luam nrog lawv cov GLP-1 analog liraglutide (Victoza), ua tiav kev muag khoom thoob ntiaj teb ntawm $ 3.2 nphom hauv 2016 txij thaum nws pib xyoo 2009. Nrog tas sij hawm ntawm patents rau liraglutide tebchaw, generic kws tuam txhab uas muag yog nyob ze saib xyuas lub khw no. Txhawm rau tiv thaiv qhov xwm txheej no, Novo Nordisk tau npaj cov tiam tom ntej liraglutide, uas yog semaglutide. Structureally, semaglutide hloov 8 txoj hauj lwm alanine ntawm GLP-1(7-37) saw nrog Aib, hloov 34 txoj hauj lwm arginine nrog lysine, thiab txuas ib qho octadecanoic acid fatty acid saw rau 26 txoj hauj lwm lysine. Piv rau liraglutide, semaglutide muaj cov roj fatty acid ntev dua, ua rau nws cov hydrophilicity. Txawm li cas los xij, semaglutide tau hloov kho nrog luv-chain polyethylene glycol (PEG), ua kom nws cov hydrophilicity. Kev hloov kho PEG tsis tsuas yog tso cai rau nws nruj nreem khi rau albumin, npog qhov chaw cleavage ntawm DPP-4, tab sis kuj txo lub raum tso tawm, yog li ncua nws ib nrab-lub neej thiab ua tiav cov txiaj ntsig ntev. Kev soj ntsuam qhia tias Ozempic xav tias yuav yog ib qho ntawm cov tshuaj muag zoo tshaj plaws hauv 2017. Novo Nordisk kwv yees tias nws qhov muag yuav ncav cuag $ 2.2 nphom los ntawm 2022. Tib lub sijhawm, Novo Nordisk tseem tab tom tsim kho qhov ncauj formulation ntawm semaglutide ntxiv rau nws. txoj haujlwm ua thawj coj hauv kev kho mob ntshav qab zib.
Hauv cov ntsiab lus, semaglutide yog GLP ua haujlwm ntev -1 analog nrog kev ua tau zoo hauv kev kho mob ntshav qab zib hom 2. Nws tau pom tias muaj txiaj ntsig zoo dua liraglutide. Los ntawm nws cov qauv tshwj xeeb thiab kev hloov kho, suav nrog cov saw roj fatty acid ntev dua thiab kev hloov kho PEG, semaglutide ua kom pom kev txhim kho hydrophilicity, nce ib nrab-lub neej, thiab lub sijhawm ua haujlwm ntev. Nws daim ntawv lag luam hu ua Ozempic.
yog koj xav tauSemaglutide hmoov CAS 910463-68-2, pls xav tias dawb hu rau peb txhua lub sijhawm. peb yuav teb koj asap.
peb cov ntaub ntawv tiv tauj:
E-mail: sales@yihuipharm.com
Tel: 0086-29-89695240
WeChat lossis WhatsApp: 0086-17792415937