Mazdutide 5mg / vial Txhim kho Metabolic Health thiab Tswj qhov hnyav

Mazdutide 5mg / lub raj mis qhia

Kev tshawb fawb-qib triple receptor agonist peptide|Ua nyob rau hauv Suav teb, lub ntiaj teb thawj GCGR / GLP-1R / GIPR triple agonist, 5mg / vial

Hom npeTom ntej: Mazdutide (IBI362)

Kev tshawb fawb thiab kev loj hlob codeSIB 362

Hom qauv: Ntev- ua yeeb yam fusion peptide raws li kev ua kom zoo dua qub OXM

Hom phiaj: Glucagon receptor (GCGR) + glucagon-zoo li peptide-1 receptor (GLP-1R) + glucose-dependent insulinotropic peptide receptor (GIPR)

Molecular hnyav: kwv yees 4112.5 Da

Purity: Ntau dua lossis sib npaug li 99.0% (UPLC xeem)

Qhov tshwm sim: Dawb lyophilized hmoov

Cia: Khaws khov ntawm -20℃deb ntawm lub teeb. Tom qab thawing, refrigerate ntawm 2-8 degrees. Tsis txhob rov qab khov-thaw cycles.

Core zoo thiab muaj nuj nqi

lub ntiaj teb thawj GLP-1R / GCGR / GIPR triple agonistnws tus kheej tsim nyob rau hauv Tuam Tshoj kom nkag mus rau hauv kev kho mob theem, sawv cevib tiam tshiab ntawm kev kho mob kev xaiv nyob rau hauv lub tshav pob ntawm cov kab mob metabolic. Los ntawmib txhij ua kom peb qhov tseem ceeb metabolic receptors ntawm tib - qib molecule, nws ua tiavKev tswj hwm thiab kev sib koom ua ke ntawm cov metabolism hauv lub zog, qabzib homeostasis, thiab lipid metabolism. Hauv kev tshawb fawb ua ntej thiab soj ntsuam ntawm kev rog rog, ntshav qab zib hom 2, thiab tsis yog - cawv fatty siab kab mob / tsis yog- cawv steatohepatitis, nws tau pom tiasKev poob phaus zoo dua thiab kev txhim kho metabolic zoo dua piv rau cov uas twb muaj lawm - phiaj GLP-1 tshuaj, uaib qho cuab yeej ua rau kev tshawb nrhiav kab mob metabolic thiab kev txhim kho tshuaj tshiab.

✅ Triplesynergistic mechanism:

GLP-1R Excitement:

Muaj zog ntshav qab zib txo cov nyhuv: Nws txhawb nqa cov tshuaj insulin secretion hauv qabzib -raws li txoj kev, txhim kho - cell functions, thiab inhibits glucagon.

Central qab los noj mov: Ua rau ntawm hypothalamus los tsim kom muaj kev noj qab haus huv zoo thiab txo cov calories kom tsawg.

Ncua lub plab khoob: ntxiv kom satiety thiab slows down assorption.

GCGR Kev Zoo Siab:

Qhov tseem ceeb nce kev siv hluav taws xob: activates daim siab metabolism, tsub kom basal metabolic tus nqi, thiab ua tiav "active rog hlawv".

Targeted txo cov rog intrahepatic: Txhawb nqa fatty acid oxidation nyob rau hauv daim siab, tshwj xeeb yog txhim kho hepatic steatosis, thiab coj kev cia siab tshiab rau kev kho mob ntawm NASH.

Txhim kho cov ntshav lipid profile: Tswj lipoprotein metabolism thiab txo qis triglycerides.

GIPR txaus siab:

Txhim kho qhov browning ntawm cov ntaub so ntswg adipose: txhawb nqa thermogenesis hauv cov ntaub so ntswg adipose dawb thiab nce kev siv zog.

Synergistic txhim kho ntawm insulin rhiab heev: Txhim kho cov tshuaj insulin- txhawb nqa cov nyhuv ntawm GLP-1 thiab txhim kho cov tshuaj insulin hauv cov ntaub so ntswg adipose.

Muaj peev xwm central appetite kev cai sib koom ua ke: Synergistic nrog GLP-1 txoj hauv kev, nws tuaj yeem ua kom zoo dua qhov qab los noj mov.

✅OriginalSuav tshawb fawb thiab kev loj hlob zoo:

Lub tswv yim tsim qauv molecular: Raws linatural OXM (gastrin) ib ntus, dhausite- qhia cov amino acid hloov pauv thiab C18 fatty acid side chain modification, qhov kev ua piv txwv ntawm triple receptors thiab cov yam ntxwv pharmacokinetic tau ua kom zoo dua qub, ua tiav ntev - noj ib zaug ib lim tiam.

Ua CMC txheej txheem:

High -kev ua tau zoo biosynthesis: SivSuav hamster zes qe menyuam (CHO) cell qhia system, siab - tawm los thiab siab - ruaj khov recombinant ntau lawm tiav.

Proprietary purification txheej txheem: Kev sivntau -qib chromatography ua ke (affinity, ion exchange, hydrophobic, molecular sieve)thev naus laus zis, ob qho khoom lag luam-txog impurities (xws li polymers thiab fragments) thiab txheej txheem -txog impurities (tus tswv tsev proteins thiab DNA) raug tshem tawm nruj heev.

Precise zoo tswj: Advanced technologies xws lithim rov qab-theem UPLC, qhov loj me ntawm chromatography, loj spectrometry, thiab ncig dichroism spectroscopy yog siv los xyuas kom meej purity Ntau dua los yog sib npaug rau 99.0%, cov ntsiab lus monomer Ntau dua los yog sib npaug rau 98.5%, raug cov qauv siab, thiab ruaj khov ua haujlwm lom.

Kev kawm zoo:

Kev txheeb xyuas kev ua ub no: Cov kev ua agonistic ntawm cAMP ntawm GLP-1R, GCGR thiab GIPRtau txheeb xyuas los ntawm cov xov tooj ntawm tes -raws li cAMP muaj nuj nqi thwmsim los xyuas kom meej triple agonistic ua tau zoo.

Kev ruaj ntseg zoo: Muab cov ntaub ntawv kawm zoo sib piv rau cov khoom xyaw tshuaj nquag (APIs) los ntawm kev tshawb fawb ntxov thiab kev loj hlob mus rau kev siv tshuaj kho mob.

Kev txhawb nqa cov ntaub ntawv kho mob: Theem II kev sim tshuaj hauv Suav teb pom tias Mazdutide tau zoo dua li dulaglutideHauv kev poob phaus thiab tswj ntshav qab zib hauv cov neeg rog rog thiab cov neeg mob ntshav qab zib hom 2, ua kom pom qhov muaj peev xwm kho tau zoo.

✅ khoomNta:

Triple target synergy: Ib qho molecule npog peb txoj hauv kev loj hauv metabolic, uas ua rau muaj kev sib koom ua ke kho mob thiab muaj peev xwm loj.

Muaj zog poob phaus thiab txo cov ntshav qab zib: Cov ntaub ntawv preclinical thiab kho mob tau lees paub tias nws muaj peev xwm txo qhov hnyav thiab txhim kho cov metabolism.

Ntev - ua yeeb yam thiab yooj yim: Qhov ua tau zoo ntev - txhawb nqa tsim qauvib zaug -ib lub lim tiamkev tswj hwm subcutaneous, txhim kho kev tshawb fawb yooj yim thiab ua raws li tus neeg mob.

Daim ntawv qhia kev siv thiab cia

1. Kev kho dua tshiab thiab kev npaj:

Cov kuab tshuaj tshwj xeeb:

Cov sterile reconstitution nrog rau diluent(cov tshuaj tsis haum nrog pH ntawm kwv yees li 7.4-8.0) yuav tsum tau siv.

Kev siv cov ntsev tsis zoo uas tsis tau lees paub, dej rau kev txhaj tshuaj, lossis lwm yam kev daws teeb meem yog txwv nruj heev., raws li nws yuav cuam tshuam rau solubility thiab stability ntawm lub sij hawm ntev - ua peptide.

Tus txheej txheem npaj:

Maj mam txhaj 1.0 mL ntawm qhov tshwj xeeb diluent raws phab ntsa sab hauv ntawm lub vial.

Maj mam tiglub vial horizontally nyob rau hauv xib-teg ntawm koj txhais tes tsawg kawg yog 2-3 feeb kom txog rau thaumib qho ntshiab, tsis muaj xim mus rau xim daj me ntsis yog tsim. Kev tshee tshee, tshee, lossis vortexing yog txwv tsis pubkom tsis txhob tsim cov npuas lossis ua rau cov protein denaturation thiab sib sau ua ke.

5 mg/mlua tau.

Yog xav tau dilution, thov sivtib lub siab diluentrau theem nrab dilution thiab maj mam invert mus sib tov.

Cov ntsiab lus tseem ceeb kom nco ntsoov:

Txoj kev npaj yuav tsum tau ua nyob rau hauv ib qho chaw huv si.

Cov tshuaj reconstituted yuav tsum tau sivhauv 1 teev.

Ua ntej kev tswj hwm,yuav tsum tau kuaj pom. Kev daws yuav tsum yog qhov tseeb thiab tsis muajpom hais, fibers, los yog discoloration.

2. Cia tej yam kev mob:

Unreconstituted lyophilized hmoov:

Khaws khovntawm -20℃± 5 degree, deb ntawm lub teeb, thiab nyob rau hauv nws thawj ntim.

Nyob rau hauv cov xwm txheej no, lub sij hawm siv tau yog teem caij tentativelyua 24ay.

Rau ntev - khaws cia ntev, nws raug nquahu kom khaws cia ntawm-80 degree.

Reconstituted tshuaj daws:

Yog tias tsis siv tam sim ntawd, nws tuaj yeem ua taumuab tso rau hauv tub yees ntawm 2-8℃tsis pub ntau tshaj 24 teev.

Tsis txhob khov cov kev daws teeb meem.

Kev thauj mus los:

Dej khov qhuav (-78 degree)yuav tsum tau siv rau kev thauj mus los los xyuas kom muaj cov saw hlau txias thoob plaws hauv tag nrho cov txheej txheem.

Lub ntim yuav tsum muaj cov cuab yeej ntsuas kub.

3. Kev tshawb fawb thiab kev npaj ua ntawv thov:

Preclinical tsiaj qauv:

Nyiam tus qauv:

Khoom noj khoom haus-induced rog (DIO) nas/rats: tus qauv tseem ceeb rau kev ntsuam xyuas kev txhim kho hauvlub cev hnyav, lub cev muaj pes tsawg leeg, kev noj zaub mov, thiab kev siv zog.

Zucker Diabetic Obese (ZDF) naslos yogdb/db nas: ntsuam xyuas kev txhim kho hauvNtshav qabzib, insulin, glycated hemoglobin, thiab insulin rhiab heev.

Nonalcoholic steatohepatitis (NASH) qauv(xws li choline-tsis muaj siab- noj zaub mov muaj roj, AMLN noj, STAM qauv): soj ntsuamdaim siab rog cov ntsiab lus, cov qhab nia mob, ballooning degeneration, thiabrov qab cuam tshuam ntawm fibrosis.

Dosage regimen:

Txoj kev pom zoo: txhaj tshuaj subcutaneous.

Dosage reference(xav tau kev ua kom zoo raws li tus qauv tshwj xeeb):

Tsawg- pawg koob tshuaj: 0.01 - 0.05 mg/kg

Cov koob tshuaj nruab nrab: 0.05 - 0.2 mg/kg

Siab - pawg koob tshuaj: 0.2 - 1.0 mg/kg

Kev siv ntau zaus: Raws li nws qhov ntev - ua yeeb yam, nws tuaj yeem tsim los tswj hwmib zaug ib lub lim tiam.

Kev soj ntsuam thiab kev ntsuam xyuas:

Core endpoints: Lub cev hnyav, noj zaub mov, ceev cov ntshav qabzib, thiab qhov ncauj qhov ncauj qhov ncauj qhov ncauj (OGTT).

Metabolic ntsuas: plaub cov ntshav lipid tsis, siab enzymes, siab triglyceride cov ntsiab lus, thiab qib insulin.

Histopathology: Daim siab H&E staining, Sirius liab staining (kev ntsuam xyuas ntawm steatosis, o, thiab fibrosis); Dawb / xim av tsom xam cov ntaub so ntswg adipose.

Lub zog metabolism: Indirect calorimetry yog siv los ntsuas kev siv hluav taws xob thiab kev ua pa ntawm lub ntsws.

Mechanism ntawm kev kawm ua:

Receptor pharmacology: Qhov kev sib raug zoo (KD) thiab kev xaiv rau peb lub hom phiaj tau txiav txim siab los ntawm radioligand binding assays lossis deg plasmon resonance techniques.

Kev taw qhia txoj kev: Tshawb xyuas nws lub peev xwm los qhib cov kev taw qhia qis qis xws li cAMP/PKA thiab -arrestin hauv cov kab sib txawv.

Central mechanism: Cov teebmeem ntawm cov tshuaj no ntawm cov chaw noj zaub mov hypothalamic (xws li ARC thiab PVN) thiab lub chaw sib npaug ntawm lub zog tau tshawb xyuas los ntawm kev siv cov tswv yim xws li kev tswj hwm intraventricular, tshwj xeeb hauv lub paj hlwb lesioning, thiab c-Fos immunostaining.

Peripheral metabolism: Uakev ntsuas hyperinsulin-positive glucose clamp testtxhawm rau txheeb xyuas qhov muaj txiaj ntsig zoo ntawm cov tshuaj insulin thoob plaws hauv lub cev thiab hauv ntau cov ntaub so ntswg (siab, nqaij, rog).

Molecular mechanisms: Transscriptomic thiab proteomic tsom xam ntawm cov ntaub so ntswg xws li daim siab thiab cov ntaub so ntswg adipose tau ua los qhia lawv cov kev tswj xyuas network.

4. Cov tswv yim tsim kev sim:

Tswj pab pawg teeb tsa:

Solvent tswj pawg

Ib leeg- phiaj los yog ntau- phiaj xwm pab pawg tswj hwm zoo (xws li Semaglutide, Tirzepatide).

Kev tshawb nrhiav koob tshuaj yuav tsum teeb tsa ntau pawg tshuaj los kawm txog koob tshuaj - teb kev sib raug zoo.

Vim li cas thiaj xaiv Mazdutide, ua hauv Suav teb?

A ntiaj teb- thawj cov tshuaj tshiab: Mazdutide yog Tuam Tshoj thawj zaug -hauv-chav kawm thawj qhov kev ua tiavnyob rau hauv lub teb ntawm metabolism. Xaiv cov khoom no txhais tau tias sawv ntawmlub forefront ntawm scientific kev tshawb fawb nyob rau hauv daim teb no.

Siabkho mob translational nqi: Cov khoom no tau uatxhawb nqa los ntawm ntau cov ntaub ntawv preclinical thiab kho mob. Cov txiaj ntsig kev tshawb fawb tuaj yeem txheeb xyuas sai nrog kev kho mob, thiab kev txhais lus muaj peev xwm loj heev.

Technologyyog ywj siab thiab tswj tau: Los ntawm kev tsim cov noob caj noob ces thiab kev tsim kho kab ntawm tes mus rau loj - nplai ntau lawm thiab kev tswj kom zoo, peb muajua kom tiav cov khoom ntiag tug kev txawj ntsethiabpuv -chain technology.

Zooua raws li cov qauv thoob ntiaj teb: Cov txheej txheem ntau lawm thiab cov qauv zoo ua raws li nruj me ntsisthoob ntiaj teb cGMP specifications, thiab cov ntaub ntawv ua tiav thiab txhim khu kev qha, ua tau raws qib siab - qib kev tshawb fawb thiab kev thov kev thov.

Tshawb nrhiav thiab siv cov lus qhia

Txiav -kev tshawb fawb txog cov kab mob metabolic:

Tshawb nrhiav tus ntoo khaub lig- kev sib tham thiab kev sib koom ua ke ntawm peb txoj hauv kev loj: GLP-1R, GCGR, thiab GIPR.

Txoj kev tshawb no tshawb xyuas qhov tshwj xeeb zoo thiab cov txheej txheem hauv qab ntawm triple stimulation hauv kev kho mob ntawm NASH/NASH- ntsig txog daim siab fibrosis.

Txhawm rau ntsuam xyuas nws cov txiaj ntsig ntev - cov txiaj ntsig rau cov kab mob plawv metabolic.

Kev sib piv ntawm Benchmark rau Kev Kho Mob Tshiab:

Raws li cov qauv ntsuas ntsuas rau "triple stimulant" lub tswv yim, nws yog siv los ntsuas qhov zoo ntawm lwm tus neeg sib tw tshuaj zoo sib xws.

Txhawm rau tshawb nrhiav qhov zoo tshaj plaws ntawm kev siv tshuaj thiab ntau zaus, muab cov pov thawj tseem ceeb rau kev txhim kho tom ntej.

Kev Tshawb Fawb Cov Tshuaj Precision:

Txhawm rau nrhiav biomarkers uas tuaj yeem kwv yees cov lus teb rau kev kho Mazdutide.

Txhawm rau tshawb nrhiav qhov sib txawv ntawm kev ua tau zoo hauv cov neeg mob uas muaj cov kab mob metabolic sib txawv (piv txwv li, feem ntau hepatic steatosis vs. feem ntau yog insulin tsis kam).

Preclinical/Clinical Data Reference

Preclinical: Hauv DIO qauv, Mazdutide qhiaCov teebmeem poob phaus zoo dua piv rau Semaglutide thiab Tirzepatide, thiab txo lub siab rog rog thiab txhim kho insulin tsis kam.

Phase II kev kuaj mob: Hauv cov neeg mob hnyav / rog, Mazdutide 6 mg koob tshuaj rau 24 lub lis piamua rau muaj txiaj ntsig zoo dua qhov feem pua ​​​​qhov hnyav dua li dulaglutide, nrog kev ruaj ntseg profile zoo.

Cov ntsiab lus

Mazdutide (IBI362),lub ntiaj teb thawj triple receptor agonist nkag mus rau kev kho mob, tsis yog xwbtus neeg sawv cev zoo tshaj plaws ntawm thawj cov tshuaj tshiab tsim nyob rau hauv Suav teb, tab sis kujlub cim tseem ceeb hauv lub sijhawm tshiab ntawm "ntau-kev sib koom ua ke" rau kev tshawb fawb txog kev kho mob metabolic. Nws cov ntaub ntawv ua tau zoo tshaj plaws thiab cov ntaub ntawv kho mob tau ua rau muaj kev vam khom rau kev kov yeej cov kab mob metabolic xws li rog, ntshav qab zib, thiab NASH. Xaiv Mazdutide tsim nyob rau hauv Suav teb yuav muab rau kojsiab - zoo, cov khoom xyaw nquag ua tau raws li cov qauv thoob ntiaj teb, pab koj ua tiav cov txiaj ntsig kev tshawb fawb hauv qhov kev txiav - ntug.

Xav taudab tsi, thov hu raupeb

Cim npe nrov: Mazdutide 5mg / vial zoo txhim kho metabolic noj qab haus huv thiab tswj qhov hnyav, Tuam Tshoj mazdutide 5mg / vial zoo txhim kho metabolic noj qab haus huv thiab tswj qhov hnyav manufacturers, lwm tus neeg, Hoobkas