Exenatide yog ib hom ntev - ua yeeb yam peptide active tshuaj synthesized los ntawm biomimetic technology, nrog rau cov txheej txheem tshwj xeeb ntawm kev txheeb xyuas tshuaj. Nws tshwj xeeb CAS nrhiav code yog 141758-74-9. Cov tshuaj no tau raug hloov kho nrog cov khoom siv peptide chains thiab muaj kev ruaj ntseg zoo dua hauv vitro thiab cov ntaub so ntswg tsom affinity piv rau tej yam ntuj tso plab hnyuv pancreatic stimulating agents. Nws cov khoom zoo physicochemical xws li spatial conformation thiab kev ua haujlwm pab pawg tuaj yeem tshawb nrhiav ntxiv thiab nthuav dav los ntawm kev sim physicochemical tshwj xeeb.
Sib txawv los ntawm cov txheej txheem metabolic classic ntawm cov khoom no,exenatide ntsiav tshuajmuaj kev ywj pheej vascular cov ntaub so ntswg kho muaj peev xwm thiab cov lus teb tshuaj tshwj xeeb. Tsab ntawv xov xwm no txheeb xyuas ob qho kev kho mob tshwj xeeb, uas yog cov txheej txheem ntau yam molecular ntawm cov tshuaj nquag cuam tshuam hauv vascular endothelial inflammatory kev raug mob thiab kev kho mob ntawm endothelial physiological functions, raws li zoo raws li lub hauv paus pib thiab maj mam tolerance evolution cov cai ntawm qab los noj mov cov tsos mob thiab tsis xis nyob. Nws systematically piav qhia nws cov yam ntxwv uas tsis yog metabolic tswj cov tshuaj pharmacological thiab cov yam ntxwv ntawm kev nyab xeeb hloov kho.
Peb Cov Khoom Txheej Txheem
ExenatideCOA
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| Certificate of Analysis | ||
| Compound npe | Exenatide | |
| Qib | Pharmaceutical qib | |
| CAS Nr. | 141732-76-5 | |
| Ntau | 39g | |
| Ntim txheem | PE hnab + Al foil hnab | |
| Chaw tsim tshuaj paus | Shaanxi BLOOM TECH Co., Ltd | |
| Ntau No. | 202601090034 | |
| MFG | Peb 9, 2026 | |
| EXP | Peb 8, 2029 | |
| Qauv |
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| Yam khoom | Enterprise txheem | Kev txheeb xyuas qhov tshwm sim |
| Qhov tshwm sim | Dawb los yog yuav luag dawb hmoov | Ua raws |
| Cov ntsiab lus dej | Tsawg dua lossis sib npaug li 5.0% | 0.54% |
| Poob rau ziab | Tsawg dua lossis sib npaug li 1.0% | 0.42% |
| Hnyav Hlau | Pb Tsawg dua lossis sib npaug li 0.5ppm | N.D. |
| Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Hg Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Cd Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Purity (HPLC) | Ntau dua lossis sib npaug li 99.0% | 99.98% |
| Ib leeg impurity | <0.8% | 0.52% |
| Tag nrho microbial suav | Tsawg dua lossis sib npaug li 750cfu / g | 95 |
| E. Coli | Tsawg dua lossis sib npaug li 2MPN / g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (los ntawm GC) | Tsawg dua lossis sib npaug li 5000ppm | 500ppm ua |
| Cia | Khaws rau hauv qhov chaw kaw, tub yees, nyob rau hauv qhov chaw tsis muaj zog | |
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Pab lub cev rov tsim cov ntshav qabzib homeostasis
Cov ntshav qabzib homeostasis kho tus nqi ntawmexenatide ntsiav tshuajTsis yog ib qho kev cuam tshuam hypoglycemic nkaus xwb, tab sis yog ib qho kev pab kho ntau yam ntawm lub cev tsis zoo ntawm cov txheej txheem metabolic, pab kho nws tus kheej kev tswj cov piam thaj. Cov teebmeem tshwjxeeb tau tshwm sim hauv peb yam:
Ua ntej, kho qhov tsis sib npaug ntawm cov kev cai bidirectional ntawm cov piam thaj metabolism.
Lub homeostasis ntawm tib neeg cov ntshav qab zib yog nyob ntawm qhov sib npaug ntawm ob lub ntsiab lus tseem ceeb ntawm cov piam thaj nce thiab txo cov piam thaj. Qhov teeb meem tseem ceeb ntawm cov neeg mob ntshav qab zib hom 2 tsis yog tsuas yog nce cov ntshav qab zib xwb, tab sis qhov ua rau muaj ntshav qabzib nce cov metabolism hauv txoj kev thiab tsis ua haujlwm ntawm kev tswj hwm endogenous thiab sib npaug. Cov tshuaj no tuaj yeem xaiv cov txheej txheem ua kom tsis zoo ntawm cov piam thaj hauv cov metabolism, ua rau muaj kev cuam tshuam cov piam thaj tsis muaj zog, tsim kho qhov chaw kho mob rau lub cev tsis muaj zog ntawm cov piam thaj hauv lub cev, thiab maj mam rov ua kom muaj zog ntawm ob lub cev metabolism, tsis yog cia siab rau sab nraud quab yuam kom yuam cov ntshav qab zib tsawg.
Secondly, alleviate lub compensatory lub nra ntawm pathological metabolism hauv daim siab.
Lub sij hawm ntev hyperglycemia tuaj yeem ua rau lub siab nyob rau hauv siab - siv lub zog metabolic kev ntxhov siab, cuam tshuam lub siab lub hauv paus metabolic atherosclerosis, thiab ua rau muaj kev puas tsuaj rau cov metabolism hauv kev ua haujlwm thiab rov ua rau cov ntshav qabzib ntau dua.
Cov tshuaj no tuaj yeem txo qhov tsis muaj txiaj ntsig endogenous qab zib synthesis ua haujlwm hauv daim siab, txo qis kev ntxhov siab hauv lub siab ntawm lub siab, thiab maj mam rov ua kom lub cev ua haujlwm ntawm lub siab ua haujlwm ntawm lub siab cov piam thaj metabolism, kho lub cev lub cev muaj peev xwm tswj cov suab thaj.
Thirdly, txiav tawm lub voj voog metabolic vicious mediated los ntawm cov ntshav qab zib siab.
Kev tsim cov piam thaj ntau dhau ntawm endogenous yuav ua rau muaj kev cuam tshuam ntawm metabolic hauv lub cev, ua rau lub cev kaw - lub voj kab mob ntawm "cov piam thaj metabolism tsis zoo, hyperglycemia, thiab lwm yam kab mob metabolic". Cov tshuaj no thaiv cov txheej txheem tsis xws luag ntawm gluconeogenesis, thaiv qhov cuam tshuam tsis tu ncua ntawm endogenous hyperglycemia, rhuav tshem lub voj voog tsis zoo, thiab muab qhov chaw nyob ruaj khov rau kev kho tus kheej ntawm lub cev endocrine kev tswj hwm lub cev thiab lub cev metabolic muaj nuj nqi, yog li ua tiav lub luag haujlwm tseem ceeb ntawm kev pab kho ntshav qabzib homeostasis.
Multi-dimensional mechanism ntawm exenatide hauv inhibiting endothelial o thiab kho endothelial physiological muaj nuj nqi
Lub vascular endothelium, raws li ib txheej ntawm cov hlwb ua haujlwm npog lub vascular lumen, yog lub cev tseem ceeb ntawm lub cev thiab cov kab mob lom neeg uas tswj hwm lub homeostasis ntawm lub vascular ib puag ncig thiab tiv thaiv cov kab mob vascular degenerative. Cov kab mob metabolic nyob rau lub sijhawm ntev hauv lub cev tuaj yeem ua rau qis qis - qib kev ntxhov siab nyob rau hauv lub vascular phab ntsa, ua rau muaj kev ua haujlwm tsis zoo ntawm endothelial cell, thaiv kev puas tsuaj rau kev ncaj ncees, thiab txo qis vasodilation muaj nuj nqi, maj mam ua rau ntau yam teeb meem vascular.Exenatide ntsiav tshuajtuaj yeem ua tiav txoj cai tiv thaiv kev puas tsuaj ntawm vascular endothelium los ntawm plaub qhov ntev ntawm kev ywj pheej: inflammatory blockade, oxidative stress nyem, barrier remodeling, thiab functional activation, raws li Toth tshwj xeeb receptor dependent txoj kev. Lawv ua tiav kho qhov cuam tshuam vascular microenvironment. Cov kev tshwj xeeb ntawm kev ua yog raws li nram no:
01. Txiav tawm qhov kev sib kis ntawm cov kab mob endothelial thiab tshem tawm cov kab mob inflammatory erosion:
Nyob rau hauv cov metabolic abnormalities, lub nuclear transcription factor Tonglu nyob rau hauv vascular endothelial hlwb tau ua kom muaj kev txawv txav, uas ua rau muaj qhov txawv txav ntawm ntau yam pro-cov kab mob inflammatory mediators thiab cell adhesion molecules, txhawb cov peripheral lub cev tiv thaiv kab mob kom adhere thiab infiltrate lub endothel kev raug mob. Cov tshuaj peptide no tuaj yeem raug khi rau lub hom phiaj receptors rau ntawm qhov chaw ntawm cov kab mob endothelial cell membranes, thaiv cov kev hloov pauv nuclear thiab cov txheej txheem nthuav dav ntawm cov teeb liab inflammatory, downregulate cov synthesis thiab tso tawm ntawm pro- cov yam ntxwv mob xws li qog necrosis factor thiab interleukin tsev neeg los ntawm molecular qhov chaw, ua rau tsis muaj zog ntawm vascular adhesion thiab adhesion molecular adhesion. ntawm lub cev tiv thaiv kab mob, txiav tawm cov kab sib kis ntawm cov kab mob inflammatory cascade tshwm sim, thiab tshem tawm cov kev yaig thiab kev puas tsuaj ntawm cov kab mob inflammatory rau vascular endothelium.
02.Dissolve endothelial oxidative kev nyuaj siab puas tsuaj thiab txhim kho cell ciaj sia taus:
High metabolic load induces ntau ntau tiam ntawm reactive oxygen hom nyob rau hauv vascular endothelial hlwb, rhuav lub dynamic tshuav ntawm lub cev oxidative thiab antioxidant systems, inducing endothelial cell oxidative puas thiab nce apoptosis tus nqi, uas yog ib qho tseem ceeb ua rau endothelial dysfunction. Exenatide tuaj yeem ua kom muaj cov kab mob antioxidant endogenous hauv lub cev, txhim kho cov kev ua haujlwm lom neeg ntawm cov tshuaj tua kab mob antioxidant hauv cov hlwb endothelial, tshem tawm cov pa oxygen dawb radicals ntau dhau, thiab txo cov txheej txheem cellular puas tsuaj los ntawm lipid peroxidation. Nyob rau tib lub sijhawm, nws tuaj yeem txo qis kev qhia theem ntawm pro apoptotic proteins, txhim kho kev ciaj sia ntawm cov hlwb endothelial, txo cov kev ntxhov siab oxidative-induced endothelial cell apoptosis thiab kev ua haujlwm poob qis, thiab tsim kom muaj kev ruaj ntseg cellular survival microenvironment rau kho cov ntaub so ntswg endothelial.
03.Reconstructing tus qauv ntawm vascular endothelial barrier thiab kho nws txoj kev ncaj ncees:
Kev mob o thiab oxidative puas tuaj yeem cuam tshuam cov qauv kev sib txuas ntawm cov kab mob endothelial, ua rau muaj qhov txawv txav ntawm cov hlab ntsha endothelial barrier. Cov tshuaj phem tuaj yeem nkag mus rau hauv vascular interstitium yooj yim, ua rau muaj kev hloov pauv xws li thickening thiab hardening ntawm phab ntsa vascular.Exenatide ntsiav tshuajcan target and regulate the synthesis and arrangement of endothelial cell junction proteins, repair damaged cell tight junction structures, reduce abnormal permeability of vascular endothelium, block the infiltration and deposition of peripheral harmful components into subendothelial tissues, reshape the physical barrier function of vascular endothelium, and build a basic defense line for vascular homeostasis at the structural level.
04. Ua kom lub endothelial vasodilation tswj txoj hauv kev thiab hloov kho vascular physiological muaj nuj nqi:
Kev noj qab haus huv vascular endothelium tuaj yeem tsim kho thiab tso tawm cov vasodilatory mediators, tswj cov vascular contraction thiab so rhythms. Kev poob qis ntawm cov neeg nruab nrab synthesis muaj nuj nqi ntawm cov kab mob endothelial puas tuaj yeem ua rau muaj teeb meem xws li vascular txhav thiab txwv kev so. Exenatide tuaj yeem qhib txoj hauv kev tshwj xeeb ntawm cov txheej txheem endothelial, txhim kho cov synthesis efficiency thiab bioavailability ntawm vasodilators xws li nitric oxide, zoo txo vascular du leeg nro, txo vascular txhav, txhim kho vascular hemodynamic xwm txheej, maj mam rov zoo li qub physiological secretion thiab tswj kev ua haujlwm ntawm vascular endothelium, thiab thim rov qab pathological vascular.
Lub laj thawj tshwm sim ntawm qhov tsis zoo tshwm sim ntawm kev poob qab los noj mov thiab maj mam ua rau lub cev tsis zoo
Kev tsis qab los noj mov yog cov lus teb tshwj xeeb tshaj plaws ntawm somatic hauv kev kho mob thaum ntxov ntawm exenatide, uas yog cov tsos mob me me mus rau nruab nrab thiab thim rov qab cov tsos mob tsis xis nyob, tsis muaj kev pheej hmoo ntawm kev puas tsuaj loj. Qhov tshwm sim ntawm cov tshuaj tiv thaiv tsis zoo no tsis yog tshwm sim los ntawm kev puas tsuaj rau cov tshuaj toxicity, tab sis los ntawm physiological adaptation cov tshuaj tiv thaiv tshwm sim los ntawm cov tshuaj tsom kev tswj ntawm central thiab peripheral metabolic sensing txoj kev. Nrog rau kev ncua sij hawm ntawm lub voj voog tshuaj, lub cev tuaj yeem maj mam txhim kho kev yoog raws, thiab cov tsos mob tsis xis nyob yuav txo qis thiab ploj mus. Cov txheej txheem induction thiab cov cai kam rau ua tuaj yeem txheeb xyuas hauv peb qhov loj:
Kev ua haujlwm ib ntus hloov kho ntawm lub hauv paus kev tswj hwm kev noj zaub mov
Cov tshuaj peptide no tuaj yeem nkag mus rau hauv cov ntshav- lub paj hlwb teeb meem thiab tsom mus rau lub chaw tswj hwm kev noj zaub mov hypothalamic, cuam tshuam hauv kev sib kis ntawm kev noj qab haus huv ntsig txog neural signals. Nyob rau hauv thawj theem ntawm kev siv tshuaj, cov tshuaj yuav inhibit thiab txhawb kev sib kis ntawm cov zaub mov paj hlwb, thaum txhim kho qhov rhiab heev ntawm satiety hlab ntsha txoj kev, reshaping lub cev noj zaub mov pib pib, ua rau satiety teeb liab ua ntej, tsis muaj zog kev tshaib kev nqhis, thiab thaum kawg ua rau ib tug txo nyob rau hauv luv luv {{2} lub hom phiaj ntawm appetite thaum ntxov.
Transient deviation ntawm peripheral gastrointestinal perception atherosclerosis
Ntxiv nrog rau kev tswj hwm hauv nruab nrab, exenatide tuaj yeem kho lub plab zom mov peristalsis atherosclerosis thiab visceral kev nkag siab muaj peev xwm, ua kom lub plab zom mov tsis zoo, thiab ua kom lub sijhawm ntev ntawm kev nkag siab ntawm plab hnyuv. Nyob rau hauv thawj theem ntawm kev siv tshuaj, lub cev tsis tuaj yeem hloov kho sai sai rau cov kev hloov pauv ntawm lub cev, ua rau muaj qhov seem seem txaus siab thiab txo qis kev xav noj. Cov kev cai no tsuas yog kev hloov pauv ntawm lub cev thiab yuav tsis ua rau muaj kev puas tsuaj rau cov kab mob hauv plab hnyuv thiab peristaltic muaj nuj nqi.
Kev rov pib dua ntawm metabolic homeostasis hauv lub cev txhawb nqa kev ua siab ntev ntev
Nyob rau lub sijhawm ntev - noj tshuaj, lub cev lub cev metabolic maj mam hloov mus rau hauv nruab nrab thiab peripheral txoj kev hloov pauv los ntawm cov tshuaj, tsim ib qho kev hloov pauv hloov pauv. Lub chaw noj zaub mov hypothalamic yuav rov pib dua lub teeb liab kev nkag siab, ua rau muaj kev cuam tshuam ntawm cov tshuaj tsis muaj zog ntawm cov hlab ntsha noj, thiab cov kab mob plab kuj tuaj yeem hloov mus rau cov peristaltic tshiab thiab khoob khoob khoob khoob khoob khoob khoob khoob khoob khoob khoob khoob khoob khoob khoob khoob khoob khoob khoob khoob khoob khoob khoob khoob khoob khoob khoob khoob. Raws li lub cev metabolic homeostasis tau rov qab los, qhov pib ua kom qab los noj mov maj mam txo qis, ua rau cov tshuaj tiv thaiv tsis tau ntev -cov teebmeem tsis zoo xws li kev noj zaub mov tsis zoo.
Cov ntaub ntawv
Liu Siyuan, Zhou Hang Kawm txog cov txheej txheem ntawm GLP-1 Receptor Agonist Mediated Steady State Repair of Vascular Endothelial Cells thiab Nws Clinical Vascular Protective Value [J]. Kawm Pharmaceutical Research, 2024, 31 (6): 412-417
Battistoni A, Piras L, Tartaglia N. Molecular mechanisms ntawm endothelial tiv thaiv los ntawm glucagon-zoo li peptide-1 receptor agonists hauv metabolic vascular disorders[J]. Frontiers in Clinical Medicine, 2025, 12: 166968.
Chen Muyang Kev Ntsuam Xyuas ntawm qhov kev zam ntawm kev hloov pauv ntawm plab hnyuv thiab noj cov tshuaj tiv thaiv tsis zoo nyob rau theem pib ntawm peptide hypoglycemic tshuaj [J]. Phau ntawv Journal of Rational Clinical Use, 2023, 16 (19): 89-92
EXENATIDE (https://drugs.ncats.io/drug/9P1872D4OL)
FAQ
AstraZeneca txiav tawm ob qho tib si ntawm exenatide (Byetta thiab Bydureon BCise) raws li kev txiav txim siab ua lag luam. Qhov kev tshem tawm no tsis yog tshwm sim los ntawm teeb meem kev nyab xeeb tshuaj; es, cov tshuaj tau ntsib kev ua lag luam floundering thiab poob qhov chaw kom yooj yim dua, tshiab dua - tiam GLP-1 kev kho mob
Cov tshuaj tiv thaiv tsis zoo no nthuav tawm qhov sib txawv ntawm tus kheej, thiab tsis yog txhua tus neeg siv tshuaj yuav muaj cov tsos mob tsis qab los noj mov. Qhov tshwm sim thawj zaug yog siab dua nyob rau hauv cov tib neeg uas muaj kev cai lij choj rhiab heev thiab mob hnyav metabolic atherosclerosis. Nyob rau tib lub sijhawm, lub voj voog kev ua siab ntev ntawm lub cev txawv ntawm ib tus neeg mus rau ib tus neeg, thiab cov neeg siv feem ntau tuaj yeem ua tiav cov metabolic homeostasis adaptation nyob rau hauv 2 mus rau 4 lub lis piam ntawm kev noj tshuaj tas mus li, nrog cov tsos mob qeeb qeeb; Lub sij hawm kam rau ntawm ib tug me me ntawm cov tib neeg lub cev rhiab heev tej zaum yuav ntev me ntsis, tab sis tag nrho nws yog thim rov qab thiab yuav tsis ua rau muaj kev noj qab haus huv tsis zoo lossis teeb meem kev noj zaub mov tsis txaus.
Exenatide muaj cov khoom lag luam ywj pheej rau kev kho thiab tiv thaiv - cov teebmeem ntawm cov hlab ntsha endothelium, thiab tuaj yeem siv nws cov teebmeem ntawm nws tus kheej yam tsis muaj kev cia siab rau kev tswj hwm cov piam thaj hauv cov metabolism. Cov tshuaj no tuaj yeem khi ncaj qha rau cov receptors tshwj xeeb ntawm cov kab mob vascular endothelial, pib txoj kev qhia tshwj xeeb rau kev tiv thaiv - mob, antioxidant, thiab kho qhov teeb meem. Txawm tias tsis muaj kev tswj hwm metabolic, nws tseem tuaj yeem thaiv cov kab mob ntev ntev rau vascular endothelium thiab txhim kho vasodilation muaj nuj nqi, uas yog nws qhov tshwj xeeb pharmacological zoo dua piv rau cov tshuaj hypoglycemic. Nws tuaj yeem cuam tshuam cov kab mob vascular degenerative tshwm sim los ntawm cov kab mob metabolic hauv lub hom phiaj.
Cim npe nrov: Tuam Tshoj exenatide ntsiav tshuaj manufacturers, lwm tus neeg
