Semaglutide peptide 10 mgyog ib tug revolutionary glucagon-zoo li peptide-1 (GLP{10}}1) analogue. Nws qhov koob tshuaj 10- milligrams yog qhov ua tau zoo hauv kev tswj hwm kev rog thiab kev kho mob ntshav qab zib. Los ntawm kev ua raws li cov tshuaj hormones GLP-1 hauv tib neeg lub cev, nws tuaj yeem ncua kev ua pa ntawm plab, ua kom qab los noj mov, thiab txhawb nqa cov tshuaj insulin secretion, yog li ua kom muaj zog thiab txhawb nqa kev poob phaus thiab tswj cov ntshav qab zib. Piv nrog rau cov tshuaj qis dua ua ntej, 10-milligram formulation muab cov tshuaj muaj zog dua thiab siv tau ntev dua, tso cai rau cov neeg mob kom ua tiav cov tshuaj ntshav ruaj khov nrog tsuas yog ib qho tshuaj subcutaneous ib lub lis piam. Cov ntaub ntawv kho mob tau lees paub tias qhov koob tshuaj no, thaum ua ke nrog kev cuam tshuam hauv kev ua neej, tuaj yeem pab cov neeg mob feem ntau poob ntau dua 15% ntawm lawv qhov hnyav thiab txhim kho cov kab mob plawv thiab cov kab mob metabolic. Nws cov txheej txheem tsim khoom nruj ua kom muaj kev ruaj ntseg thiab kev ua haujlwm lom neeg ntawm cov saw peptide, tab sis qhov ntau npaum li cas yuav tsum tau maj mam titrated raws li kev qhia ntawm tus kws kho mob kom txo tau qhov kev pheej hmoo ntawm kev mob plab hnyuv, muab cov kev kho mob tshiab thiab muaj txiaj ntsig zoo rau kev tswj xyuas qhov hnyav mus ntev.
Peb Cov Khoom
Semaglutide COA
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| Certificate of Analysis | ||
| Compound npe | Semaglutide | |
| CAS Nr. | 910463-68-2 | |
| Ntau | 105kg ua | |
| Ntim txheem | 25kg / nruas | |
| Chaw tsim tshuaj paus | Shaanxi BLOOM TECH Co., Ltd | |
| Ntau No. | 20250206015 | |
| MFG | 06 Peb 2025 | |
| EXP | 06 Peb 2028 | |
| Qauv | N/A | |
| Yam khoom | Enterprise txheem | Kev txheeb xyuas qhov tshwm sim |
| Qhov tshwm sim | Dawb hmoov | Ua raws |
| Cov ntsiab lus dej | Tsawg dua lossis sib npaug li 5.0% | 3.8% |
| Poob rau ziab | Tsawg dua lossis sib npaug li 1.0% | 0.35% |
| 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) | >99% | 99.13% |
| Ib leeg impurity | <0.8% | 0.40% |
| Tag nrho microbial suav | Tsawg dua lossis sib npaug li 750cfu / g | 80 |
| 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 | 200 ppm |
| Cia | Khaws rau hauv qhov chaw kaw, tsaus, thiab qhuav hauv qab 2-8 degree | |
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Semaglutide peptide(ib tug hluavtaws peptide compound) yog ib tug derivative ntawm glucagon -zoo li peptide-1 (GLP-1) receptor agonist. Cov khoom siv tshuaj lom neeg ntawm nws cov qauv 10mg tuaj yeem tshawb pom los ntawm cov khoom xws li cov qauv molecular, solubility, stability, thiab cov txheej txheem ntawm kev hloov kho lom neeg.
Cov yam ntxwv ntawm cov qauv molecular
Semaglutide yog tsim los ntawm 31 amino acids thiab muaj cov qauv molecular ntawm C₁₈₇H₂₉₁N₄₅O₅₉, nrog rau qhov hnyav molecular ntawm kwv yees li 4113 Da. Nws cov qauv zoo ib yam li ntawm ntuj GLP-1, tab sis nws ua kom muaj kev ruaj ntseg los ntawm kev hloov ntawm ob qho tseem ceeb amino acids:
8 txoj hauj lwm alanine (Ala) yog hloov los ntawm 2-aminoisobutyric acid (Aib)
Kev taw qhia ntawm Aib tuaj yeem tiv thaiv qhov degradation los ntawm dipeptidyl peptidase-4 (DPP-4). DPP-4 yog ib qho enzyme uas tshwm sim hauv lub cev uas ua rau sai sai uas tsis hloov kho GLP-1, ua rau lub neej ib nrab ntawm 1-2 feeb xwb. Txawm li cas los xij, cov qauv stereoscopic ntawm Aib cuam tshuam qhov enzyme cleavage site ntawm DPP-4, txuas ntxiv ib nrab-lub neej ntawm Semaglutide mus rau kwv yees li 7 hnub.
Lub 34th lysine (Lys) yog hloov los ntawm arginine (Arg)
Cov saw tseem ceeb ntawm Arg txhim kho txoj kev sib raug zoo nrog GLP-1 receptor thiab ua kom zoo dua qhov kev faib tawm molecular, ntxiv stabilizing cov tshuaj hauv lub cev.
Tsis tas li ntawd, Semaglutide txuas 18-carbon atom fatty acid saw (C₁₈) mus rau lysine sab saw ntawm txoj hauj lwm 26, ua tiav covalent khi los ntawm valeric acid txuas caj npab. Qhov kev hloov kho no ua rau nws khi rau plasma albumin, txo lub raum tshem tawm thiab yog li ncua lub sijhawm ua haujlwm.
Solubility kev ua tau zoo
Lub solubility ntawm Semaglutide cuam tshuam loj heev los ntawm nws cov qauv molecular.
Polar pawg txhim kho dej solubility:Cov pawg polar nyob rau hauv cov molecule, xws li carboxyl pawg (-COOH) thiab amino pawg (-NH₂), tuaj yeem tsim hydrogen bonds nrog dej molecules, uas ua rau muaj ntau dua solubility hauv dej ntshiab.
Fatty acid side chain cuam tshuam qhov sib npaug ntawm qhov sib npaug:Ntev - chains fatty acid side chains yog hydrophobic thiab yuav txo tau tag nrho cov solubility. Txawm li cas los xij, los ntawm kev hloov kho PEG (xws li luv luv -chain polyethylene glycol txuas), qhov hydrophilicity ntawm Semaglutide yog txhim kho, sib npaug ntawm hydrophobic thiab hydrophilic zog.
pH-nyob ntawm kev sib cais:Nyob rau hauv acidic los yog nruab nrab ib puag ncig (xws li pH 7 aqueous tov), lub solubility ntawm Semaglutide tuaj yeem ncav cuag 1 mg / mL, ua rau nws yooj yim rau kev npaj cov tshuaj txhaj tshuaj lossis kev npaj qhov ncauj. Txawm li cas los xij, nyob rau hauv huab cua pH (xws li cov kua qaub uas muaj zog lossis cov hauv paus muaj zog), nws cov solubility yuav txo qis, thiab ntev - yuav tsum zam kom raug.
Stability mechanism
Kev ruaj ntseg ntawm Semaglutide yog ua tiav los ntawm ntau yam kev hloov kho tshuaj:
Resistance rau enzymatic hydrolysis
Tom qab Aib hloov lub ntuj Ala, DPP-4 tsis tuaj yeem paub txog nws qhov chaw enzymatic cleavage, yog li tiv thaiv cov tshuaj los ntawm degradation.
Albumin khi
Tom qab cov fatty acid sab saw khi rau plasma albumin, ib qho chaw ruaj khov yog tsim, txo cov filtration clearance ntawm cov tshuaj nyob rau hauv lub raum. Albumin tseem tuaj yeem npog qhov chaw enzymatic cleavage site ntawm DPP-4, txuas ntxiv rau ib nrab-lub neej.
Kub thiab lub teeb rhiab heev
Semaglutide peptidenyob rau hauv hmoov daim ntawv yuav tsum tau muab cia rau ntawm -20℃los tiv thaiv molecular degradation los yog tsim ntawm impurities. Lub sij hawm ntev raug kub los yog lub teeb yuav ua rau cov roj fatty acids tawg, txo cov tshuaj ua haujlwm.
Oxidation stability
Cov sulfur atoms nyob rau hauv lub molecule (xws li methionine residues) tej zaum yuav oxidized, tab sis xws li cov tshuaj tiv thaiv yuav ua tau zoo inhibited los ntawm nruj cia tej yam kev mob (xws li zam lub teeb thiab noo noo).
Chemical hauv paus ntawm kev hloov pauv kev ua haujlwm lom neeg
Kev ua haujlwm lom neeg ntawm Semaglutide stems los ntawm nws qhov tshwj xeeb khi rau GLP-1 receptor, thiab cov txheej txheem no tso siab rau tus qauv tsim ntawm nws cov qauv tshuaj:
Receptor binding domain
Nws -Aib-Glu sequence ntawm N-terminus ntawm lub molecule yog qhov chaw tseem ceeb khi rau GLP-1 receptor. Kev taw qhia ntawm Aib tsis cuam tshuam qhov kev sib khi muaj peev xwm ntawm cheeb tsam no; xwb, nws stabilizes tus conformation thiab txhim khu kev affinity.
Kev cai ntawm kev hloov pauv
Lub Arg-Gly-Arg-Gly ib ntus ntawm C-terminus yog koom nrog hauv lub teeb liab hloov tom qab receptor activation. Nws cov nqi xa tawm yog qhov ua tau zoo nrog lub ntuj GLP-1, kom ntseeg tau tias cov tshuaj tuaj yeem ua rau cov tshuaj insulin secretion thiab inhibit glucagon secretion.
Ntev - lub sij hawm mechanism
Kev khi ntawm fatty acid sab saw rau albumin tsis tsuas yog ncua ib nrab ntawm - lub neej tab sis kuj ua rau cov tshuaj tso tawm hauv lub cev los ntawm "slow-} tso tawm cov nyhuv", tswj cov ntshav cov tshuaj kom ruaj khov, yog li txo qhov kev siv tshuaj ntau zaus (ib zaug hauv ib lub lis piam).
Cov nyhuv synergistic ntawm bioactive hloov kho
Semaglutide peptide 10 mgyog ua tiav cov txheej txheem metabolic zoo los ntawm nws cov kev hloov pauv bioactive hauv 10mg formulation los ntawm ntau yam kev sib koom ua ke. Lub hauv paus ntsiab lus nyob rau hauv kev sib xyaw ua ke ntawm amino acid hloov pauv thiab fatty acid sab saw hloov kho, uas sib koom ua ke txhim kho cov tshuaj stability, receptor affinity, thiab nyob rau hauv vivo ncig lub sij hawm.
Amino acid hloov pauv txhim kho enzyme tsis kam thiab receptor khi
Cov qauv tsim molecular ntawm semaglutide suav nrog ob qhov tseem ceeb amino acid hloov pauv: 8 txoj haujlwm alanine (Ala) yog hloov los ntawm -aminoisobutyric acid (Aib), thiab 34th lysine (Lys) yog hloov los ntawm arginine (Arg). Kev taw qhia ntawm Aib thaiv cov enzyme cleavage site ntawm dipeptidyl peptidase-4 (DPP-4) los ntawm steric hindrance, ua rau cov tshuaj tiv thaiv rau enzymatic degradation kwv yees li 100 npaug, yog li zam qhov tsis xws luag ntawm ntuj GLP-1 tau sai sai hauv lub cev. Kev hloov pauv ntawm Arg optimizes molecular nqi faib thiab txhim kho kev sib raug zoo nrog GLP-1 receptor, kom ntseeg tau tias cov tshuaj muaj peev xwm ua kom cov receptor zoo ntawm qhov tsis tshua muaj siab thiab ua rau cov teeb liab xa mus. Qhov kev hloov kho dual no tsis tsuas yog ua rau lub sijhawm ntev ntawm cov tshuaj ib nrab-lub neej, tab sis kuj ua rau lub zog ruaj khov ntawm receptor binding conformation, txhim kho qhov tshwj xeeb ntawm cov teeb liab hloov.
Fatty acid side-kev hloov pauv cov saw tau ua tiav ntev- lub sijhawm tso tawm
Sab 26th lysine - saws ntawm Semaglutide yog covalently txuas mus rau 18-carbon fatty acid saw (C18) los ntawm succinic acid linker. Qhov kev hloov kho no ua rau nws tsis yog -covalently khi rau plasma albumin, tsim ib qho chaw ruaj khov. Albumin, raws li cov khoom muaj protein ntau tshaj plaws hauv lub cev, tuaj yeem tiv thaiv cov tshuaj los ntawm kev ua kom lub raum tsis zoo thiab lub raum tshem tawm, thiab tib lub sijhawm, los ntawm "txhim kho qhov tso tawm", tso cai rau cov tshuaj tso tawm tsis tu ncua hauv lub cev. Kev sim cov ntaub ntawv qhia tau hais tias qhov kev hloov kho no txuas ntxiv ib nrab- lub neej ntawm Semaglutide mus rau kwv yees li 7 hnub, txhawb nqa ib zaug - kev tswj hwm txhua lub lim tiam, txhim kho kev ua raws li tus neeg mob. Ntxiv mus, cov kev taw qhia ntawm fatty acid side-chain kuj optimizes cov tshuaj tis ntawm lub cell daim nyias nyias los ntawm kev ua kom nws lipophilicity, ntxiv dag zog rau receptor binding efficiency.
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Synergistic cuam tshuam ua rau ntau- lub hom phiaj kev txhim kho metabolic
Kev hloov kho cov txheej txheem ntawm semaglutide ua rau cov txheej txheem metabolic network tswj los ntawm ib txoj hauv kev (GLP-1 receptor activation), ua tiav "ib qho- tua ntau yam txiaj ntsig" synergistic nyhuv:
Kev tswj ntshav qabzib
Cov tshuaj no txhawb kev tsim cov tshuaj insulin hauv cov piam thaj hauv cov ntshav -ib yam li nyob thiab inhibits glucagon tso tawm, ua tiav cov ntshav qab zib kom tsawg.
Kev tswj qhov hnyav
Los ntawm kev ua kom lub paj hlwb thiab lub paj hlwb nuclei, nws ncaj qha tswj lub chaw noj mov hauv hypothalamus, txo kev tshaib kev nqhis thiab ncua kev ua pa ntawm plab, yog li txo cov zaub mov noj.
Kev tiv thaiv kab mob plawv
Kev txhim kho endothelial muaj nuj nqi, txo cov ntshav siab, thiab tiv thaiv- cov teebmeem inflammatory ua ke txo qhov kev pheej hmoo ntawm atherosclerosis, txo qis qhov tshwm sim ntawm cov xwm txheej mob plawv loj (MACE).
Kev tiv thaiv raum
Los ntawm kev txo cov ntshav qab zib, ntshav siab, thiab qhov hnyav, nws ua rau qeeb ntawm kev mob ntshav qab zib nephropathy thiab txo cov qib proteinuria.
Clinical validation thiab tshawb fawb tus nqi
Cov kev tshawb fawb SUSTAIN tau lees paub tias kev kho mob Semaglutide tuaj yeem txo hemoglobin A1c (HbA1c) los ntawm 1.5%-1.8% hauv cov neeg mob ntshav qab zib hom 2, txo qhov hnyav li 4-6 kg, thiab ib txhij txhim kho cov ntsuas metabolic xws li ntshav siab thiab qib lipid. Hauv kev tshawb fawb, nws tau dav siv los ua tus qauv molecule los tshawb txog cov teebmeem ntawm peptide fatty acidation ntawm cov roj ntsha ib nrab-lub neej thiab cov neeg txais kev sib raug zoo, muab cov tswv yim sim rau kev hloov kho ntawm lwm cov peptide molecules. Piv txwv li, Semaglutide derivatives sau nrog fluorescence lossis radioactivity tuaj yeem txiav txim siab qhov kev sib khi kinetic tsis muaj, muab cov ntaub ntawv ntau rau kev tshuaj xyuas tshuaj.
FAQ
1. Dab tsi yog qhov tseem ceeb ntawm 10mg semaglutide?
Nws yog tsuas yog siv rau kev kho mob ntshav qab zib hom 2 thiab pab tswj qhov hnyav. Raws li kev noj zaub mov nruj thiab kev tawm dag zog, nws tuaj yeem txo cov ntshav qab zib kom zoo thiab txo lub cev hnyav.
2. Yuav siv thiab khaws cia li cas?
Nws feem ntau yog siv los ntawm kev txhaj tshuaj subcutaneous ib zaug ib lub lim tiam. Cov koob tshuaj yuav tsum maj mam nce los ntawm qib qis tshaj raws li tus kws kho mob cov lus qhia. Cov vials uas tsis tau qhib yuav tsum muab cia rau hauv tub yees ntawm 2-8 degree; Tom qab qhib, lawv tuaj yeem khaws cia rau hauv chav tsev kub tab sis yuav tsum tsis txhob raug rau qhov khov los yog lub hnub ci ncaj qha.
3. Cov kev phiv tshwm sim yog dab tsi?
Cov tsos mob tshwm sim feem ntau yog mob plab hnyuv xws li xeev siab thiab raws plab, uas feem ntau yog qis thaum lub cev yoog. Nws yog ib qho tseem ceeb kom paub txog qhov tsis tshua muaj tab sis muaj kev pheej hmoo loj, xws li pancreatitis thiab kab mob biliary. Thov sab laj nrog kws kho mob ua ntej siv los ntsuam xyuas tej contraindications.
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