Shaanxi BLOOM Tech Co., Ltd. yog ib qho ntawm cov tuam ntxhab thiab cov muag khoom ntawm adipotide peptide hauv Suav teb. Txais tos rau kev lag luam wholesale bulk zoo adipotide peptide muag ntawm no los ntawm peb lub hoobkas. Kev pabcuam zoo thiab tus nqi tsim nyog muaj.
Adipotide peptideyog ib qho hluavtaws peptidomimetic compound tsim los tsom thiab cuam tshuam cov ntshav muab rau cov ntaub so ntswg adipose, yog li txhawb kev txo cov rog. Cov peptide no tshwj xeeb khi rau txwv tsis pub, cov protein ntau tau hais tawm ntawm cov hlab ntsha adipocytes, ua rau apoptosis hauv cov hlwb endothelial uas txhawb nqa cov hlab ntsha. Los ntawm kev xaiv tsis zoo vascularization nyob rau hauv cov rog deposits, Adipotide induces hypoxia thiab nutrient deprivation, ua rau lub shrinkage ntawm adipose ntaub so ntswg. Cov kev tshawb fawb hauv cov qauv tsiaj tau pom tias nws ua tau zoo hauv kev txo lub cev hnyav thiab rog rog yam tsis muaj kev cuam tshuam rau lub cev, ua rau nws muaj kev vam meej rau kev tshawb fawb metabolic. Lub peptide cov txheej txheem ntawm kev ua yog txawv ntawm cov kev cai ib txwm, raws li nws tsom mus rau vasculature es tsis ncaj qha hloov adipocyte muaj nuj nqi los yog central metabolic txoj kev. Adipotide lub hom phiaj cuam tshuam qhia txog nws qhov muaj peev xwm siv tau hauv cov tshuaj kho tsiaj thiab cov ntawv thov kev noj qab haus huv tsiaj, tshwj xeeb tshaj yog rau kev tswj kev rog rog-txog cov xwm txheej hauv cov tsiaj txhu lossis tsiaj txhu. Cov kev tshawb fawb ntxiv txuas ntxiv mus tshawb txog nws qhov ntev - lub sijhawm kev nyab xeeb profile thiab cov tswv yim pom zoo rau ntau hom.
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Adipotide hmoov COA
Mechanism of Action thiab Core Characteristics
Adipotide Peptideyog ib qho kev sim peptide tshuaj. Nws cov qib molecular yog CKGGRAKDC-GG-D(KLAKLAK)₂. Nws induces apoptosis los ntawm kev tsom mus rau vascular endothelial hlwb ntawm cov ntaub so ntswg adipose, yog li ua tiav cov rog txo. Txoj kev txiav txim tuaj yeem muab faib ua ob theem:
Vascular targeting theem:Cov peptide ntu (CKGGRAKDC) tshwj xeeb khi rau qhov txwv tsis pub receptors ntawm qhov chaw ntawm adipose cov ntaub so ntswg vascular endothelial hlwb, thaiv cov teeb liab angiogenesis.
Apoptosis theem:Cov ntu tom kawg (D(KLAKLAK)₂) yog lub xovtooj ntawm tes - nkag mus rau peptide uas nqa cov hydrophobic amino acid sib lawv liag mus rau hauv cytoplasm, cuam tshuam cov mitochondrial membrane muaj peev xwm, ua kom txoj hauv kev caspase, thiab inducing programmed cell tuag.
Cov kev sim tsiaj tau pom tias cov txheej txheem no tuaj yeem txo cov ntshav mus rau cov ntaub so ntswg adipose los ntawm 70% - 90%, thiab adipocytes yuav pib qhov kev pab cuam apoptosis li ntawm 48 - 72 teev vim hypoxia thiab cov khoom noj tsis txaus.
Tsis yog -Human Application Scenarios thiab Dose Regimens
Tam sim no, kev tshawb fawb ntawm Adipotide feem ntau yog tsom rau cov qauv tsiaj rog rog (xws li nas thiab rhesus liab) thiab cov qauv kab mob metabolic (xws li ua ntej- liab liab). Nws tseem tsis tau pom zoo siv rau tib neeg. Cov hauv qab no yog cov txheej txheem sim ua raws li cov cai:
Obese nas qauv
Noj: 0.1 - 0.5 mg/kg lub cev hnyav, txhaj tshuaj subcutaneous txhua hnub.
Lub Sij Hawm: Kev tswj hwm tsis tu ncua rau 4 lub lis piam, tom qab ntawd tshem cov tshuaj rau 4 lub lis piam rau kev soj ntsuam.
Cov nyhuv:
Qhov hnyav poob los ntawm 25% - 30% (txo tsis tu ncua tom qab tshem tawm cov tshuaj);
Lub plab rog txo los ntawm 40% - 50%;
Cov ntshav ntshav triglyceride txo qis los ntawm 35%.
Mechanism pov thawj: Los ntawm fluorescently sau npe peptides, nws tau lees paub tias lawv nyiam nyob hauv cov hlab ntsha ntawm cov ntaub so ntswg dawb es tsis yog cov leeg lossis daim siab.
Rhesus liab rog qauv
Noj: 0.3 - 0.75 mg/kg lub cev hnyav, txhaj tshuaj subcutaneous 3 zaug hauv ib lub lis piam.
Sijhawm: 9 lub lis piam ntawm kev tswj hwm + 4 lub lis piam ntawm kev tshem tawm tshuaj.
Cov nyhuv:
Qhov hnyav nruab nrab poob los ntawm 11% (nruam txo tom qab tshem tawm cov tshuaj);
Cov roj ntim tau txo los ntawm 39%;
Kev yoo mov ntshav qabzib txo qis los ntawm 15% - 20%, insulin rhiab heev los ntawm 40%.
Kev txhim kho metabolic: Kev soj ntsuam ntawm kev txhim kho cov piam thaj hauv cov ntshav 2 - 3 hnub tom qab kev tswj hwm, ua ntej qhov hnyav hloov pauv, qhia tias nws tuaj yeem txhim kho cov metabolism los ntawm kev tswj hwm cov tshuaj hormone secretion hauv cov ntaub so ntswg adipose (xws li adiponectin nce, leptin txo).
Pre-mob ntshav qab zib liab qauv
Kev Siv: 0.5 mg / kg lub cev hnyav, txhaj tshuaj subcutaneous txhua hnub.
Sijhawm: 2 lub lis piam ntawm kev tswj hwm.
Cov nyhuv:
Insulin rhiab heev nce 50%;
Lub siab triglyceride cov ntsiab lus txo los ntawm 30%;
Cov gene qhia profile ntawm cov ntaub so ntswg adipose pom tau hais tias inflammatory-cov noob caj noob ces (xws li TNF- , IL-6) tau downregulated, thiab lipid metabolism-txog cov noob (xws li PPAR-, LPL) tau upregulated.
Kev khiav hauj lwm Specifications thiab ceev faj
Kev npaj thiab khaws cia
Kev kho dua tshiab: Npaj nrog cov tshuaj tsis huv ib txwm saline lossis PBS, nrog rau qhov siab ntawm 1-5 mg / mL. Tsis txhob tuav lub zog kom tiv thaiv peptide degradation.
Cia: Khaws rau luv- lub sij hawm (hauv 1 lub lis piam) ntawm 4℃; rau ntev - lub sij hawm cia, aliquot thiab khov ntawm -20℃los yog -80℃kom tsis txhob rov khov thiab thawing.
Txoj kev tswj hwm
Kev txhaj tshuaj subcutaneous: nyiam xaiv lub plab lossis sab hauv ntawm sab nraub qaum. Qhov ntim txhaj tshuaj yuav tsum tsis pub tshaj 0.2 mL / kg kom txo qis hauv zos.
Intravenous txhaj: Tsuas yog rau kev tshawb fawb pharmacokinetic. Maj mam txhaj tshuaj (Ntau dua lossis sib npaug li 5 feeb) txhawm rau tiv thaiv cov ntshav siab sai.
Cov ntsuas ntsuas
Lub cev hnyav thiab lub cev rog: ntsuas lub cev hnyav txhua lub lim tiam. Siv DEXA lossis MRI los ntsuas cov rog.
Metabolic Parameters: Tsis tu ncua kuaj ntshav qabzib ceev, insulin, thiab lipids (TG, HDL / LDL).
Kev Ntsuam Xyuas Kev Nyab Xeeb: Saib xyuas lub siab thiab lub raum kev ua haujlwm (ALT, AST, BUN, Cr) thiab saib xyuas qhov chaw txhaj tshuaj liab, kev hloov hauv qab los noj mov, thiab lwm yam rau cov kev mob tshwm sim.
Kev tshawb fawb txwv thiab ceeb toom txog kev pheej hmoo
Hom txawv
Cov nas thiab primates muaj qhov sib txawv rhiab heev rau Adipotide. Rhesus liab xav tau koob tshuaj ntau dua kom ua tiav cov txiaj ntsig zoo sib xws li cov nas, tejzaum nws yog vim qhov sib txawv ntawm kev txwv tsis pub muaj cov lus qhia ceev.
Tsis paub Ntev -Tsev Teeb Meem
Lub sijhawm soj ntsuam ntev tshaj plaws rau kev sim tsiaj yog 6 lub hlis. Tsis muaj cov ntaub so ntswg rov tsim dua lossis metabolic compensatory rebound, tab sis ntev -lub sij hawm kev nyab xeeb xav tau kev txheeb xyuas ntxiv.
Immune Response Risk
Kev tswj hwm rov qab tuaj yeem ua rau muaj cov tshuaj tiv thaiv kab mob, ua rau txo qis kev ua tau zoo. Cov chaw sim yuav tsum muaj cov ntsiab lus tshawb xyuas cov tshuaj tiv thaiv kab mob (piv txwv li, 4, 8, thiab 12 lub lis piam tom qab tswj hwm).
Kev Ua Raws Cai
Tsis yog-kev sim tib neeg yuav tsum ua raws li 3R lub hauv paus ntsiab lus (hloov, txo, thiab ua kom zoo dua) kom ntseeg tau tias tsiaj noj qab haus huv thiab zam kev txom nyem tsis tsim nyog.
Cov Lus Qhia Txog Kev Tshawb Fawb Yav Tom Ntej
Kev Kho Mob Ua Ke
Tshawb nrhiav kev siv Adipotide ua ke nrog GLP-1 receptor agonists, SGLT-2 inhibitors, thiab lwm yam tshuaj metabolic los txhim kho kev ua tau zoo lossis txo cov kev mob tshwm sim ntawm koob tshuaj.
Targeted Delivery System
Tsim cov nanoparticle lossis liposome encapsulation thev naus laus zis los txhim kho kev ruaj ntseg ntawm peptide thiab txo qis kev raug mob.
Mechanism Deepening
Kawm txog qhov cuam tshuam ntawm Adipotide ntawm cov nqaij ntshiv adipose, plab hnyuv microbiota, thiab lwm yam kab mob metabolic kom qhia txog txoj kev ua tiav rau kev txhim kho cov metabolism.
Xaus
Adipotide peptideqhia tau hais tias muaj peev xwm tseem ceeb rau kev txo cov rog thiab kev txhim kho metabolic hauv cov kev tshawb fawb tsis yog - tib neeg. Txawm li cas los xij, nws daim ntawv thov yuav tsum nruj me ntsis ua raws li kev sim tshwj xeeb, ua kom zoo npaum li cas raws li cov yam ntxwv ntawm hom, thiab tsis tu ncua saib xyuas kev nyab xeeb thiab ntev - cov teebmeem. Nyob rau hauv lub neej yav tom ntej, nrog breakthroughs nyob rau hauv kev xa khoom technology thiab kev tshawb fawb mechanism, qhov peptide yuav tsum muab cov tswv yim tshiab rau kev kho mob rog rog thiab kab mob metabolic.
Adipotide Peptide(FTPP) yog ib qho kev sim hluavtaws peptide nrog cov txheej txheem CKGGRAKDC-GG-D(KLAKLAK)₂. Nws induces apoptosis nyob rau hauv cov ntaub so ntswg adipose vascular endothelial hlwb, yog li ua tiav cov roj txo. Cov txheej txheem tsim khoom suav nrog cov kauj ruam tseem ceeb xws li peptide synthesis, purification, tswj kom zoo, thiab kev ruaj ntseg ruaj khov. Cov kev ntsuam xyuas hauv qab no yog ua los ntawm qhov kev xav ntawm cov ntsiab lus technical, txheej txheem ntws, thiab cov qauv zoo.
Lub hauv paus ntsiab lus: Molecular Design Targeting Fat Blood Vessels
Cov qauv molecular ntawm Adipotide muaj ob ntu, uas sib koom ua tiav nws cov phiaj xwm apoptotic:
Lub hom phiaj Module (CKGGRAKDC)
Cov kab ke no ua tiav lub hom phiaj los ntawm kev khi tshwj xeeb rau cov txwv tsis pub receptors ntawm qhov chaw ntawm adipose cov ntaub so ntswg vascular endothelial hlwb. Prohibitin yog ib qho kev txuag ntawm daim nyias nyias cov protein ntau uas tau nthuav tawm hauv adipose thiab qog vascular endothelium, tab sis tsis tshua muaj tshwm sim hauv lwm cov ntaub so ntswg, muab Adipotide siab xaiv.
Apoptosis Module (D (KLAKLAK)₂):
Cov kab ke no yog lub xov tooj ntawm tes - nkag mus rau peptide uas, tom qab nqa hydrophobic amino acids rau hauv cytoplasm, cuam tshuam cov mitochondrial membrane muaj peev xwm, ua kom txoj hauv kev caspase, thiab induces programmed cell tuag. Qhov kev tsim no ua rau Adipotide kom meej meej lub hom phiaj ntawm cov hlab ntsha adipose, tom qab ntawd thaiv cov ntshav los ntawm cov apoptosis hauv zos, ua rau adipocytes tuag vim hypoxia thiab cov khoom noj tsis txaus.
Txheej Txheem Flow: Precise Control los ntawm Synthesis mus rau cov khoom tiav
Kev tsim cov Adipotide yuav tsum muaj cov tshuaj sib xyaw ua ke thiab kev ua kom huv huv kom paub meej tias nws cov haujlwm thiab kev ruaj ntseg:
Khoom-phase synthesis (SPPS)
Fmoc tiv thaiv pab pawg tswv yim tau txais yuav maj mam txuas cov peptide saw ntawm cov cab cab. Cov kauj ruam tseem ceeb suav nrog:
Deprotection: Siv cov tshuaj piperidine tshem tawm cov pab pawg Fmoc, nthuav tawm cov amino pawg;
Coupling: Ntxiv activated amino acids (xws li HBTU / DIPEA system) los tsim peptide bonds;
Txiav: Tom qab kev sib txuas ua tiav, siv trifluoroacetic acid (TFA) txiav cov polypeptide los ntawm cov resin thiab tshem tawm cov saw hlau tiv thaiv cov pab pawg ib txhij.
Cov theem no yuav tsum muaj kev tswj xyuas nruj ntawm cov tshuaj tiv thaiv (xws li qhov kub thiab txias, pH, thiab lub sijhawm tshuaj tiv thaiv) kom tsis txhob muaj kev sib tw los yog tsim los ntawm - cov khoom.
Purification thiab kev txheeb xyuas
High-kev ua tau zoo kua chromatography (HPLC): cais lub hom phiaj peptide los ntawm impurities los ntawm kev thim rov qab -theem chromatography kem (xws li C18), nrog rau qhov purity feem ntau ncav cuag ntau dua lossis sib npaug li 98%;
Mass spectrometry analysis (MS): Paub meej tias qhov hnyav molecular yog raws li tus nqi tsim (qhov hnyav molecular ntawm Adipotide yog 2611.41 g / mol);
Amino acid sequence tsom xam: Txheeb xyuas qhov tseeb raws li Edman degradation lossis tandem loj spectrometry.
Txias- txheej txheem ziab
Txhawm rau txhim kho kev ruaj ntseg, cov purified polypeptide yuav tsum tau dehydrated los ntawm khov - ziab (Lyophilization). Cov txheej txheem no suav nrog:
Ua ntej- khov: Ceev ceev cov tshuaj kom qis dua -40℃los tsim cov dej khov sib xws;
Sublimation drying: Cua sov nyob rau hauv qis siab kom ncaj qha hloov dej khov rau hauv roj;
Kev soj ntsuam kom qhuav: Ntxiv cua sov kom tshem tawm cov seem seem, ua rau cov khoom kawg uas muaj cov ntsiab lus noo noo feem ntau tsawg dua 2%.
Lub khov -qhuav Adipotide tshwm li cov khoom dawb, xoob xoob, uas yooj yim khaws thiab rov ua dua- yaj.
Cov Qauv Zoo: Cov Lus Qhia Tseem Ceeb rau Kev Ua Haujlwm thiab Kev Nyab Xeeb
Kev tsim cov Adipotide yuav tsum ua kom tau raws li cov kev cai hauv qab no:
Purity thiab impurity tswj
Peak purity:HPLC nrhiav kom tau ntau dua lossis sib npaug li 98%, zam kev cuam tshuam los ntawm impurities ntawm kev ua haujlwm lossis ua rau muaj kev tiv thaiv kab mob;
Cov khoom muaj feem xyuam:Cov ntsiab lus ntawm peptides ploj lawm, oxidized peptides, thiab lwm yam yuav tsum tau tswj hwm (feem ntau<1%);
Residual kuab tshuaj:Cov seem ntawm cov kuab tshuaj organic xws li TFA yuav tsum ua raws li ICH cov lus qhia (xws li<500 ppm).
Kev ruaj ntseg lav
Ntim:Siv cov roj inert (xws li nitrogen) rau kev sau kom tsis txhob oxidation;
Cia tej yam kev mob:luv-lub sij hawm (hauv 1 lub lis piam) yuav tsum khaws cia ntawm 4℃; rau ntev - khaws cia, cov khoom yuav tsum tau aliquoted thiab khov ntawm -20℃los yog -80℃kom tsis txhob rov khov-thawing uas yuav ua rau degradation;
Reconstitution txheej txheem:Npaj siv sterile physiological saline los yog PBS, nrog ib tug concentration ntawm 1-5 mg / mL. Tsis txhob tuav lub zog kom tiv thaiv peptide tawg.
Kev txheeb xyuas cov haujlwm
Txheeb xyuas nws cov kev ua haujlwm lom neeg los ntawm kev sim ntawm tes (xws li inducing apoptosis ntawm adipose vascular endothelial hlwb) los yog tsiaj qauv (xws li poob phaus hauv cov nas rog rog thiab txo cov roj ntim) kom ntseeg tau tias txhua pawg ntawm cov khoom ua tau raws li qhov xav tau.
Daim ntawv thov kev cia siab thiab kev nyuaj ntawm kev tsim khoom
Kev tsim cov thev naus laus zis ntawm Adipotide muab cov cuab yeej tshiab rau kev kho cov kab mob metabolic, tab sis nws daim ntawv thov loj - tseem ntsib cov teeb meem:
Kev ua kom zoo dua tus nqi: Cov nqi ntawm cov khoom siv-theem synthesis thiab purification yog qhov siab, thiab yuav tsum tau tsim cov txheej txheem ua tau zoo dua;
Ntev- lub sij hawm ruaj khov: Kev tshawb fawb ntxiv yog xav tau nyob rau lub sij hawm ntev - lub sij hawm cia ntawm khov- cov khoom qhuav;
Hom tshwj xeeb: Qhov sib txawv ntawm qhov sib txawv ntawm cov tsiaj sib txawv rau Adipotide (xws li cov tshuaj sib txawv rau nas thiab rhesus liab) yuav tsum tau kho tshwj xeeb thaum tsim khoom.
Nyob rau hauv lub neej yav tom ntej, nrog rau kev nce qib ntawm kev xa khoom thev naus laus zis (xws li nanoparticle encapsulation) thiab cov txheej txheem synthesis, kev tsim khoom thiab kev ruaj ntseg ntawm Adipotide yuav tsum tau txhim kho, tso lub hauv paus rau nws txoj kev hloov ntawm chav kuaj mus rau kev kho mob.
Cov lus nug nquag
Dab tsi yog qhov zoo tshaj peptide rau kev rog rog?
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Cov peptides zoo tshaj plaws rau kev poob phaus yog GLP-1 agonists zoo li Tirzepatide (Zepbound, Mounjaro), Semaglutide (Wegovy, Ozempic), thiab Liraglutide (Saxenda), uas txo qis qab los noj mov thiab ua kom tag nrho, nrog Tirzepatide feem ntau suav tias ua tau zoo tshaj plaws vim nws txoj kev ua dual-1/G (GLP-IP). Lwm cov kev xaiv zoo suav nrog CJC-1295 nrog Ipamorelin thiab AOD 9604, uas txhawb kev loj hlob hormone thiab rog metabolism. Nco ntsoov nrog kws kho mob ua ntej pib kho peptide, vim lawv tuaj yeem muaj kev phiv thiab tsis haum rau txhua tus.
Lwm lub npe rau Adipotide yog dab tsi?
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Adipotide, tseem hu uaFTPP (Fat{0}}Targeted Proapoptotic Peptide), yog ib qho hluavtaws peptidomimetic compound tsim los induce apoptosis nyob rau hauv vasculature ntawm dawb adipose ntaub so ntswg xaiv.
Puas yog lub plab rog adipose ntaub so ntswg?
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Visceral rog yog intra- plab adipose ntaub so ntswgkhaws cia nyob ib ncig ntawm ob peb lub cev, nrog rau lub plab, hnyuv thiab lub siab. Kev nce hauv visceral rog ntau dua 130 cm² txhais tau tias Visceral Obesity, ib qho kev pheej hmoo loj ntawm ntau cov kab mob ntev ntawm qhov hnyav lossis BMI qib.
Cov kab mob dab tsi cuam tshuam nrog cov ntaub so ntswg adipose?
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Kev tsim cov roj hauv lub cev ntau dhau ua rau muaj kev cuam tshuam ntawm metabolic thiab kab mob, suav nrog insulin tsis kam, prediabetes, hom 2 mob ntshav qab zib mellitus (T2DM), dyslipidemia (high triglyceride thiab qis siab - ntom ntom lipoprotein cholesterol (HDL{3}}C) circulating concentrations), gout, thiab metabolic 4.
Cov ntaub so ntswg adipose puas tuaj yeem mob qog noj ntshav?
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Liposarcoma yog ib hom mob qog noj ntshav uas tsis tshua muaj tshwm sim hauv cov rog rog. Nws feem ntau pib raws li kev loj hlob ntawm cov hlwb hauv plab lossis hauv caj npab thiab ceg leeg. Tab sis liposarcoma tuaj yeem pib hauv cov rog rog nyob txhua qhov chaw hauv lub cev. Liposarcoma tshwm sim feem ntau hauv cov neeg laus, tab sis nws tuaj yeem tshwm sim rau txhua lub hnub nyoog.
Cim npe nrov: adipotide peptide, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom