Tirzepatideyog ib qho tshuaj tshiab rau kev kho mob ntshav qab zib hom 2, tshuaj formula: C209H335N61O65S. Dawb los yog yuav luag dawb hmoov, solubility tsawg heev nyob rau hauv dej, tab sis siab solubility nyob rau hauv non-aqueous solvents (xws li methanol, dimethyl sulfoxide). Nws yuav tsum tau muab cia rau hauv qhov chaw qhuav thiab txias, tsis txhob kub, av noo, lub teeb thiab khov. Nws muaj kev ruaj ntseg siab thiab tseem tuaj yeem tswj tau qhov zoo thiab kev ua haujlwm tom qab lub sijhawm ntev cia thiab kev thauj mus los.
Tirzepatide yog ib hom tshuaj tshiab rau kev kho mob ntshav qab zib hom 2, uas tuaj yeem siv los tswj cov ntshav qab zib, txo qhov hnyav thiab txhim kho kev pheej hmoo ntawm cov hlab plawv. Tshwj xeeb, kev siv tseem ceeb ntawm Tirzepatide suav nrog:
1. Txo cov ntshav qab zib: Tirzepatide tuaj yeem txo cov ntshav qab zib los ntawm kev ua kom cov insulin tso tawm, ua kom cov piam thaj los ntawm lub siab qeeb, thiab txhawb cov carbohydrate metabolism hauv cov hnyuv. Qhov no tseem ceeb heev rau kev tswj cov ntshav qab zib hauv cov ntshav qab zib.
2. Kev tswj qhov hnyav: Tirzepatide tuaj yeem txo qhov qab los noj mov thiab noj zaub mov ntawm cov neeg mob, yog li pab cov neeg mob ntshav qab zib kom tswj lawv qhov hnyav. Tsis tas li ntawd, Tirzepatide kuj tseem tuaj yeem txo cov rog rog, ntxiv kom txo tau qhov kev rog rog.
3. Txhim kho kev pheej hmoo ntawm cov hlab plawv: cov neeg mob ntshav qab zib feem ntau muaj kev pheej hmoo ntawm cov kab mob plawv. Tirzepatide tuaj yeem txhim kho kev mob plawv ntawm cov neeg mob los ntawm kev txo cov roj cholesterol, txo cov atherosclerosis thiab txhim kho lub plawv.
Feem ntau, Tirzepatide muaj ntau yam kev siv hauv kev kho mob ntshav qab zib hom 2, thiab nws cov txiaj ntsig zoo tshaj plaws tau lees paub hauv kev sim tshuaj.
Tirzepatide yog hom tshuaj peptide uas muaj peb qhov sib txawv peptides tau los ntawm cov tshuaj insulin zoo li kev loj hlob -1 receptor agonist (GLP-1), insulin, thiab glucagonstatin (GIP). Cov hauv qab no yog txoj kev hluavtaws ntawm Tirzepatide:
1. Synthesis ntawm N-terminal peptides: Ua ntej, ib qho chaw uas muaj GLP-1 receptor agonist active peptide yog npaj los ntawm cov tshuaj synthesis. Tom qab ntawd, ib qho leucine residue tau qhia ntawm N-terminus ntawm peptide siv cov txheej txheem sib xyaw ua ke.
2. Synthesis ntawm central peptides: Insulin peptides yog npaj los ntawm cov tshuaj synthesis. Kev tiv thaiv cov pab pawg siv hauv qhov kev sib txuas no suav nrog alanine, arginine, tyrosine, serine, histidine thiab cysteine.
3. Synthesis ntawm C-terminal peptides: glucagonstatin peptides tau npaj los ntawm cov tshuaj synthesis. Tiv thaiv cov pab pawg siv hauv qhov kev sib txuas no suav nrog alanine, serine, lysine thiab phenylmethoxycarbonyl.
4. Synthesis of Tirzepatide: Peb peptides tsim Tirzepatide los ntawm disulfide bonds. Cov kauj ruam no feem ntau yog ua hauv kev daws teeb meem.
Tirzepatide yog ib qho fusion protein nrog cov qauv tshuaj ntawm ntau lub molecules sib txawv. Nws cov yam ntxwv tseem ceeb ntawm cov tshuaj yog raws li nram no:
1. Cov khoom xyaw: Nws yog tsim los ntawm ob qho kev loj hlob zoo li insulin -1 receptor agonists (GLP-1 RA) thiab ib qho insulin receptor agonist (GIP RA).
2. Thermal stability: Tirzepatide muaj thermal stability zoo thiab tuaj yeem khaws cia thiab thauj ntawm qhov kub siab dua
3. Cov tshuaj tiv thaiv tshuaj: Tirzepatide muaj ntau pawg amine thiab carboxyl pawg, uas tuaj yeem ua tiav cov tshuaj tiv thaiv kab mob xws li cov tshuaj tiv thaiv condensation thiab esterification cov tshuaj tiv thaiv.
4. Solubility: Lub solubility hauv dej yog tsawg heev, tab sis cov solubility nyob rau hauv non-aqueous solvents (xws li methanol, dimethyl sulfoxide) yog siab.
Nws yuav tsum raug sau tseg tias cov no tsuas yog qee yam tshuaj lom neeg ntawm Tirzepatide, thiab nws cov khoom siv tshuaj lom neeg kuj cuam tshuam los ntawm ib puag ncig thiab lwm yam tshuaj. Cov khoom siv tshuaj tshwj xeeb xav tau kev tshawb fawb ntxiv thiab tshuaj xyuas.
Tirzepatide yog ib qho fusion protein, thiab nws cov khoom muaj zog feem ntau koom nrog ntau pawg hauv nws cov molecule, suav nrog cov amino, carboxyl thiab thiol pawg. Cov nram qab no yog cov reactive zog ntawm Tirzepatide:
1. Cov tshuaj tiv thaiv condensation: Cov amino thiab carboxyl pawg hauv Tirzepatide tuaj yeem raug cov tshuaj tiv thaiv condensation los tsim cov peptide bonds. Cov tshuaj tiv thaiv no yog ib qho ntawm cov tshuaj tiv thaiv tseem ceeb hauv kev tsim Tirzepatide protein.
2. Oxidation cov tshuaj tiv thaiv: Cov thiol pawg hauv Tirzepatide molecules tuaj yeem oxidized rau disulfide bonds los tsim cov intra-molecular los yog intermolecular cross-links los txhim kho kev ruaj ntseg ntawm nws cov qauv.
3. Cov tshuaj tiv thaiv Esterification: Cov pab pawg carboxyl hauv Tirzepatide tuaj yeem hnov mob nrog cawv los ua ib daim ntawv cog lus ester.
4. Amination cov tshuaj tiv thaiv: Cov pab pawg carboxyl hauv Tirzepatide tuaj yeem cuam tshuam nrog amine los ua ib daim ntawv cog lus amide.
5. Cov tshuaj tiv thaiv Redox: Cov amino thiab carboxyl pawg hauv Tirzepatide tuaj yeem koom nrog cov tshuaj tiv thaiv redox, xws li txo qis rau nitroso thiab amino pawg, lossis oxidized rau sulfurous acid thiab ketones.
Nws yuav tsum raug sau tseg tias cov tshuaj tiv thaiv ntawm Tirzepatide yuav cuam tshuam los ntawm ib puag ncig thiab cov khoom sib txawv, xws li nyob rau hauv acidic los yog alkaline tej yam kev mob, los yog nyob rau hauv lub xub ntiag ntawm oxidizing los yog txo cov neeg ua hauj, cov tshuaj tiv thaiv zog yuav txawv.
Tirzepatide yog ib qho tshuaj tshiab rau kev kho mob ntshav qab zib hom 2, thiab nws cov keeb kwm tshawb pom tuaj yeem tshawb pom rov qab ze li ob xyoo lawm.
1. Xyoo 2003, lub tuam txhab tshuaj Danish Novo Nordisk tau pib tshawb nrhiav cov tshuaj analogs ntawm GLP-1, ib qho tshuaj uas txhawb nqa cov tshuaj insulin. Txij thaum ntawd los, Novo Nordisk tau ua tiav ntau yam ntawm GLP-1 receptor agonists (GLP-1 RA), suav nrog Exenatide, Liraglutide thiab Semaglutide.
2. Xyoo 2011, Novo Nordisk pib tsim GIP receptor agonists (GIP RA), ib yam tshuaj uas txhawb nqa cov tshuaj insulin secretion, zoo ib yam li GLP-1. Txij thaum ntawd los, Novo Nordisk tau txuas ntxiv tsim ntau yam GIP receptor agonists, suav nrog teduglutide, semaglutide thiab lwm yam.
3. Nyob rau xyoo 2018, Novo Nordisk pib muab ob yam tshuaj, GLP-1 RA thiab GIP RA, rau hauv ib qho tshuaj, Tirzepatide. Txij thaum ntawd los, Novo Nordisk tau tshaj tawm ntau qhov kev sim tshuaj, uas tau lees paub qhov ua tau zoo ntawm Tirzepatide hauv kev txo cov ntshav qab zib, tswj lub cev hnyav, thiab txhim kho kev pheej hmoo ntawm cov hlab plawv.
4. Xyoo 2021, Novo Nordisk tau xa daim ntawv thov tshuaj tshiab rau Tirzepatide rau US FDA thiab tau txais FDA qhov kev pom zoo sai. Tam sim no, Tirzepatide tau pom zoo los ntawm ntau lub teb chaws thiab cheeb tsam xws li Tebchaws Meskas, Tebchaws Europe thiab Nyij Pooj, thiab tau dhau los ua cov tshuaj tshiab rau kev kho mob ntshav qab zib hom 2 nrog rau daim ntawv thov dav dav.
Tirzepatide, raws li cov tshuaj tshiab rau kev kho mob ntshav qab zib hom 2, muaj kev vam meej loj hlob.
Ua ntej, Tirzepatide muaj kev kho mob siab. Cov txiaj ntsig kev soj ntsuam tau pom tias piv nrog cov tshuaj kho mob ntshav qab zib niaj hnub tam sim no, Tirzepatide ua haujlwm zoo dua hauv kev txo cov ntshav qab zib, tswj lub cev hnyav, txhim kho cov hlab plawv, thiab lwm yam, thiab muaj kev txhim kho tseem ceeb ntawm cov neeg mob cov tshuaj insulin thiab kev tso tawm ntawm insulin.
Thib ob, Tirzepatide muaj kev phiv tsawg dua. Txawm hais tias Tirzepatide belongs rau kev sib xyaw ntawm ob cov tshuaj, GLP-1 RA thiab GIP RA, nws cov koob tshuaj qis thiab koob loj ua rau muaj kev pheej hmoo ntawm cov kev mob tshwm sim ntawm cov neeg mob uas siv Tirzepatide tsawg.
Thaum kawg, Tirzepatide muaj kev lag luam dav dav. Raws li kev txheeb cais, tus naj npawb ntawm cov neeg mob ntshav qab zib hauv ntiaj teb tau tshaj 460 lab, thiab kwv yees li 90 feem pua ntawm cov neeg mob ntshav qab zib yog cov ntshav qab zib hom 2. Ntxiv mus, tus naj npawb ntawm cov neeg mob ntshav qab zib tseem nce ntxiv, uas muab lub hauv paus ruaj khov rau kev ua lag luam ntawm Tirzepatide.
Raws li cov ntsiab lus, Tirzepatide muaj cov txiaj ntsig zoo, cov kev mob tshwm sim tsawg dua thiab kev cia siab rau kev lag luam dav, yog li nws txoj kev loj hlob yav tom ntej yog dav heev.