Glucagon zoo li peptide-1 (GLP-1), tseem hu ua Glucagon Zoo li Peptide-1, yog 30 amino acid peptide hormone secreted los ntawm txoj hnyuv L hlwb thiab yog ib tug tseem ceeb ntawm tsev neeg enteropancreatin. Nws yog synthesized nyob rau hauv lub L hlwb ntawm lub ileum thiab txoj hnyuv, thiab tso tawm mus rau hauv cov hlab ntsha tom qab raug txhawb los ntawm cov as-ham xws li carbohydrates thiab rog, ua rau nws ib tug natural "ntshav qab zib steward" thiab "qab los noj mov nres" nyob rau hauv tib neeg lub cev. Zaj dab neeg ntawm GLP-1 qhia txog kev hloov pauv loj hauv tag nrho cov qauv ntawm kev kho cov kab mob metabolic, txij li thaum xub thawj pom tias yog ib qho incretin mus ua ib lub hom phiaj tshuaj kub tshaj plaws thoob ntiaj teb.
1. General Specification (hauv Tshuag)
(1) API (Ntshiab hmoov)
2.Customization:
Peb yuav sib tham tus kheej, OEM / ODM, Tsis muaj hom, rau kev tshawb nrhiav kev ruaj ntseg nkaus xwb.
PIB: BM-1-187
GLP -1 7-37 CAS 106612-94-6
Cov mis mos molecular: C151H228N40O47
Molecular Luj: 3355.67
Chaw tsim tshuaj paus: BLOOM TECH Wuxi Hoobkas
Kev tshuaj xyuas: HPLC, LC-MS, HNMR
Lub khw tseem ceeb: Tebchaws Asmeskas, Australia, Brazil, Nyiv, Lub Tebchaws Yelemees, Indonesia, UK, New Zealand, Canada thiab lwm yam.
Peb muab GLP-1, thov xa mus rau lub vev xaib hauv qab no kom paub meej cov lus qhia tshwj xeeb thiab cov ntaub ntawv khoom.
Khoom siv:https://www.bloomtechz.com/synthetic-chemical/api-kev tshawb nrhiav-only/glp-1-7-37-peptide.html
Anjin GIPR cov tshuaj tiv thaiv kab mob sib txuas GLP-1 cov tshuaj tshiab AMG 133 ntxiv kev saib xyuas kev kho mob theem III kev sim tshuaj
Thaum Lub Tsib Hlis 8, 2026, Anjin tau sau npe GIPR cov tshuaj tiv thaiv kab mob sib txuas GLP-1 cov tshuaj tshiab AMG 133 (Maridebart Caffraglutide) ntawm Clinicaltrials.gov lub vev xaib rau kev saib xyuas kev kho theem III kev soj ntsuam MARITIME-SWITCH tom qab kho GLP-1.
Phase III qhov kev npaj khomob yuav tso npe rau 300 yam kev kawm thiab xav tias yuav ua kom tiav los ntawm Lub Ib Hlis 2028. Cov txheej txheem suav nrog rau Phase III kev kuaj mob no yog cov pejxeem uas muaj BMI225 (tsis muaj kev rog rog siab dua 30) thiab qhov hnyav poob ntau dua 10% tom qab kho GLP-1. Los ntawm qhov kev xav ntawm thawj qhov kawg thiab qhov kawg ntawm qhov kev ua tau zoo thib ob, lub hom phiaj ntawm theem III qhov kev sim tshuaj ntsuam xyuas no yog los tswj qhov hnyav ntawm GLP-1 txog AMG 133, uas yog, tswj kev rov qab los.
AMG 133 (Maridebart Caffraglutide) yog lub ntiaj teb thawj GIPR antibody txuas nrog GLP-1 cov tshuaj tshiab tsim los ntawm Amgen. Nws txais cov qauv tshwj xeeb ntawm GIPR antagonist antibody txuas nrog GLP-1 agonist peptide, uas txawv ntawm cov pa GLP-1 / GIP dual agonists. Nws ua tiav qhov hnyav poob los ntawm kev ua kom GLP-1 receptors los txo qis qab los noj mov thiab thaiv GIP receptors kom tsis muaj zog lipophilic.
Roche GLP-1R / GIPR dual agonist RO7795068 txhaj tau txais kev pom zoo CDE rau daim ntawv thov kev kho mob hauv tsev
Tsis ntev los no, lub vev xaib raug cai ntawm Tuam Tshoj National Center for Drug Evaluation (CDE) tau qhia tias Roche's Class 1 cov tshuaj tshiab RO7795068 txhaj tshuaj yoj yoj kev soj ntsuam daim ntawv thov tau txais kev tso cai, nrog rau cov lus qhia tau hais tias: haum rau ntev -lub sij hawm tswj qhov hnyav ntawm cov neeg mob rog rog lossis rog dhau los ntawm kev tswj kev noj zaub mov thiab ua kom muaj zog.
RO7795068 yog GLP-1R / GIPR dual agonist tsim los ntawm Carmot. Thaum Lub Kaum Ob Hlis 2023, Roche tau txais cov khoom lag luam los ntawm Carmot rau $ 3.1 billion. Lub Insight database qhia tau hais tias kev rog rog rau RO7795068 tau nce mus rau theem kho mob hauv Sichuan txawv teb chaws.
Phase I cov txiaj ntsig tau pom tias kev txhaj tshuaj subcutaneous ntawm RO7795068 ib zaug hauv ib lub lis piam (them zuj zus qhov koob tshuaj mus rau 24mg) txo tus neeg mob qhov hnyav los ntawm 22.5% (kwv yees kev ua tau zoo), thiab tsis ncav cuag qhov hnyav poob siab ntawm 48 lub lis piam.
Txoj kev tshawb fawb tau pom qhov koob tshuaj tseem ceeb - teb kev sib raug zoo ntawm kev poob phaus thiab ntau npaum li cas. Hauv kev tshuaj xyuas ntawm kev kwv yees kev kho mob, RO7795068 tau ua tiav cov placebo kho qhov hnyav ntawm 18.3% (p<0.001).
Keeb kwm Discovery
Los ntawm Lizard Saliva mus rau Nobel nqi zog
Zaj dab neeg ntawm GLP-1 tau pib nrog kev tshawb pom ntawm glucagon los ntawm Starling thiab Bayliss hauv xyoo 1902, tab sis nws tsis yog txog li peb caug xyoo dhau los uas nws lub peev xwm hypoglycemic tau tshwm sim tiag tiag.
Qhov kev tawg ntxov tshaj plaws yog los ntawm lizard - xyoo 1992, cov kws tshawb fawb tau rho tawm peptide hu ua Exenatide los ntawm qaub ncaug ntawm Gila dab. Cov peptide no muaj 53% homology nrog cov amino acid sib lawv liag ntawm tib neeg GLP-1, tab sis tuaj yeem tiv thaiv kev degradation sai los ntawm dipeptidyl peptidase-4 (DPP-4) hauv lub cev, nrog rau plasma ib nrab-lub neej txog li 2.4 teev, deb tshaj qhov tsawg dua 2 feeb ntawm natural GLP-1.
Qhov kev tshawb pom no ncaj qha ua rau lub ntiaj teb thawj GLP-1 receptor agonist tshuaj, exenatide (lub npe lag luam: Bacitracin), uas tau pom zoo rau kev ua lag luam los ntawm FDA hauv 2005.
Xyoo 2023, Svetlana Mojsov thiab Joel Habener, ob tug thawj coj hauv kev tshawb fawb GLP-1, tau txais txiaj ntsig Lasker Basic Medical Research Award nrog rau Katalin Karik ó rau lawv txoj kev koom tes rau kev tshawb pom ntawm enteropancreatin, ntxiv kev lees paub qhov tseem ceeb ntawm GLP-1 hauv cov tshuaj niaj hnub.
Xyoo 2024, Semaglutide qhov muag txhua xyoo tau tshaj $ 20 nphom, ua rau lub ntiaj teb "duab huab tais" thiab thawb GLP-1 mus rau kev lag luam siab.