Octreotide Acetate hmoovyog ib qho kev sib xyaw ua ke ntawm somatostatin. Nws yog ib qho octapeptide compound uas muaj cov amino acids txuas nrog peptide bonds. Nws cov mis molecular yog C53H74N10O13S2 • C2H4O2, CAS 83150-76-9, nrog ib tug txheeb ze molecular luj ntawm 1129.38. Vim muaj ntau yam peptide thiab thioether daim ntawv cog lus hauv nws cov qauv, nws cov khoom siv tshuaj lom neeg kuj ruaj khov thiab nws muaj qee qhov ua rau lub teeb, kub, thiab acidity. Nws yog cov kua uas tsis muaj xim los yog yuav luag tsis muaj xim tsis muaj xim vim nws cov solubility siab nyob rau hauv aqueous daws thiab cov tshuaj ruaj khov. Lub solubility hauv dej yog qhov siab, tab sis nws kuj yog yooj yim soluble nyob rau hauv feem ntau siv organic solvents xws li ethanol thiab acetone. Qhov kev solubility zoo no tso cai rau ctreotide tau yooj yim sib xyaw nrog lwm cov tshuaj lossis cov kuab tshuaj. Cov khoom siv tshuaj lom neeg muaj kev ruaj khov, tab sis nyob rau hauv cov xwm txheej hnyav xws li kub siab, muaj zog acid lossis lub hauv paus muaj zog, decomposition lossis polymerization tshwm sim tuaj yeem tshwm sim. Lub viscosity cuam tshuam los ntawm qhov kub thiab txias. Thaum tsis kub, nws viscosity yuav nce; Nyob rau hauv qhov kub thiab txias, nws viscosity yuav txo.
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Tshuaj Formula |
C51H70N10O2S2 |
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Exact Mass |
1078 |
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Molecular Luj |
1078 |
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m/z |
1078 (100.0%), 1019 (53.0%), 1020 (13.8%), 1020 (9.0%), 1021 (4.8%), 1019 (3.7%), 1020 (2.1%), 1020 (2.0%), 1019 (1.6%), 1021 (1.5%), 1022 (1.2%), 1021 (1.1%) |
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Elemental Analysis |
C, 57.74; H, 6.53; N, 13.74; O, 15.70; S, 6.29 |
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Octreotide acetate hmoovyog siv los inhibit kev loj hlob hormone, plab hnyuv thiab pancreatic peptide secretion. Hauv kev pom ntawm kev siv tshuaj ntawm cov khoom no, nws yog qhov yuav tsum tau ua kev tshawb fawb hauv vivo.
Cov kev sim tshwj xeeb yog raws li hauv qab no:
Octreotode tuaj yeem txo cov ntshav qabzib ntau ntawm cov nas rog rog hauv pawg HFD. Kev cuam tshuam Octreotode txo qis hauv cov ntshav cov tshuaj insulin ntau ntxiv; Txawm li cas los xij, qib TG, TC, FFA, ALT thiab AST tsis txo qis. Octreotode ho inhibit HOMA index. Octreotode txo ipgtt thiab ipitt AUC, tab sis tsis loj. Octreotode txhim kho cov fatty degeneration ntawm HFD induced rog rog thiab tsub zuj zuj ntawm lipid droplets nyob rau hauv PA kho HepG2 hlwb. Octreotode tuaj yeem txhawb Akt thiab GSK3 hauv HFD ntxias cov nas rog rog Phosphorylation thiab GSmRNA qhia. Piv nrog rau pab pawg kho tsheb (tswj pab pawg), octreotode txo lub cev hnyav thiab lub raum ntub dej. PAS thiab octreotode / PAS kev kho mob txo qis cAMP theem ntawm PCK nas, tab sis octreotode ib leeg tsis txo nws. Tus naj npawb ntawm PS6 cov hlwb zoo hauv octreotode / PAS pawg tau tsawg dua li ntawm pawg PAS ib leeg, yog li nws tau ua pov thawj tias cov khoom lag luam muaj qee yam cuam tshuam rau hauv plab hnyuv pancreatic secretion peptide.
Octreotide Acetate hmoovyog ib qho kev sib xyaw ua ke ntawm somatostatin.
1. Kev kho mob ntawm plab hnyuv thiab pancreatic endocrine qog:
Raws li ib qho tshwj xeeb thiab siab affinity ligand rau somatostatin receptor (SSTR), nws tuaj yeem khi rau SSTR ntawm cov qog hlwb, inhibit qhov kev loj hlob thiab kev tso tawm ntawm cov qog hlwb, thiab yog li ua lub luag haujlwm hauv kev kho mob plab hnyuv thiab pancreatic endocrine qog. Nws txoj kev ua tau zoo tau raug lees paub los ntawm ntau qhov kev sim tshuaj thiab tuaj yeem siv los kho ntau yam kab mob hauv plab thiab pancreatic endocrine qog, xws li gastrinoma, vasoactive plab hnyuv peptidoma, thiab lwm yam.
2. Txo cov tsos mob:
Nws tuaj yeem cuam tshuam kev ua haujlwm ntawm plab hnyuv thiab pancreatic endocrine qog, yog li txo cov tsos mob tshwm sim los ntawm cov qog nqaij hlav ntau dhau, xws li raws plab, mob plab, thiab plab hnyuv. Lub caij no, nws tseem tuaj yeem txo cov tsos mob xws li raws plab thiab mob plab los ntawm lwm yam laj thawj.
3. Kev kuaj mob pab:
Nws kuj tseem muaj qee yam txiaj ntsig hauv kev kuaj mob plab hnyuv thiab pancreatic endocrine qog. Piv txwv li, hauv somatostatin receptor imaging thev naus laus zis, nws tuaj yeem ua tus taug qab los pab cov kws kho mob tshawb pom qhov chaw thiab qhov loj ntawm cov qog, muab lub hauv paus rau kev tsim kho cov phiaj xwm. Tsis tas li ntawd, nws tseem tuaj yeem siv los txheeb xyuas cov theem qhia ntawm somatostatin receptors hauv cov qog hlwb, kwv yees cov lus teb kho mob thiab kev kuaj mob.
4. Kev tiv thaiv cov teeb meem:
Nws tuaj yeem cuam tshuam kev ua haujlwm ntawm plab hnyuv thiab pancreatic endocrine qog, yog li txo qhov kev pheej hmoo ntawm cov teeb meem tshwm sim los ntawm ntau cov tshuaj hormones tso tawm los ntawm cov qog, xws li hypoglycemia, dej electrolyte disorders, thiab lwm yam. Rau cov neeg mob uas twb muaj teeb meem tshwm sim, cov tsos mob kuj yuav txo tau thiab cov mob zoo tuaj.
5. Tswj cov tshuaj hormones:
Nws tuaj yeem khi rau ntau cov tshuaj hormones receptors, yog li ua lub luag haujlwm hauv kev tswj cov qib tshuaj hormones. Piv txwv li, nws tuaj yeem cuam tshuam qhov tso tawm ntawm gastrin, glucagon thiab lwm yam tshuaj hormones, uas pab tswj cov ntshav qab zib thiab txhim kho cov tsos mob ntawm ntshav qab zib. Tsis tas li ntawd, nws tuaj yeem cuam tshuam qhov tso tawm ntawm cov thyroid stimulating hormone, uas pab kho cov thyroid kab mob.
6. Kev kho mob ntawm portal hypertension hauv daim siab cirrhosis:
Nws tuaj yeem txo qhov siab ntawm cov hlab ntsha ntawm cov neeg mob uas muaj ntshav siab portal hauv daim siab cirrhosis, thiab txhim kho cov tsos mob thiab cov tsos mob tshwm sim los ntawm portal hypertension. Nws cov txheej txheem ntawm kev ua haujlwm suav nrog inhibiting qhov tso tawm ntawm cov tshuaj hormones xws li glucagon thiab vasoactive plab hnyuv peptide, nrog rau txo qis ntawm cov hlab ntsha hauv cov hlab ntsha.
7. Kev kho mob uas tsis yog-mob qog nqaij hlav qog noj ntshav:
Cov kev tshawb fawb tsis ntev los no tau pom tias nws tuaj yeem cuam tshuam kev loj hlob thiab kev tsiv teb tsaws ntawm cov tsis yog -cov qog nqaij hlav qog nqaij hlav me me, thiab ua rau lawv apoptosis. Nws cov txheej txheem ntawm kev ua haujlwm yuav cuam tshuam rau kev tswj cov teeb liab hloov txoj hauv kev thiab cov noob qhia hauv cov qog hlwb. Txawm hais tias yuav tsum muaj kev sim tshuaj ntxiv los txheeb xyuas qhov ua tau zoo ntawm kev siv ctreotide hauv kev kho mob tsis yog -mob qog noj ntshav hauv lub ntsws, qhov kev tshawb pom no muab cov tswv yim tshiab thiab txoj hauv kev kho mob ntsws cancer.
Peb yog cov chaw tsim khoomOctreotide Acetate hmoov.
Lus Cim: BLOOM TECH (Txij li xyoo 2008), ACHIEVE CHEM-TECH yog lub chaw pabcuam ntawm peb.
Octreotode acetate, tseem hu ua ctreotide hauv Suav, yog ib qho kev sib xyaw ua ke ntawm somatostatin. Cov hauv qab no yog cov txheej txheem kuaj sim rau nws cov khoom:
1. Raw khoom thiab reagents:
Yuav tsum muaj cov reagents: L-threonine, L-valine, L-tyrosine, L-glycine, L-cysteine, L-phenylalanine, glycinamide, D-mannose, acetic anhydride, thiab lwm yam.
Yuav tsum tau reagents: sodium hydroxide, hydrochloric acid, anhydrous ethanol, ether, thiab lwm yam.
2. Synthesis cov kauj ruam:
Kauj ruam 1:
Synthesize precursors ntawm somatostatin analogues. Cov kauj ruam no suav nrog kev sib txuas ntau yam amino acids hauv ib qho kev txiav txim tshwj xeeb los tsim cov qauv ntawm octapeptide. Cov kauj ruam no feem ntau yuav tsum tau siv cov pab pawg tiv thaiv los tiv thaiv cov pab pawg nquag ntawm qee cov amino acids, kom tsis txhob muaj kev cuam tshuam sab nraud thaum lub sijhawm sib txuas.
Kauj ruam 2:
Tshem tawm cov pab pawg tiv thaiv thiab tau txais cov tshuaj tiv thaiv acetylation. Nyob rau hauv cov kauj ruam no, muaj zog acid los yog lub hauv paus yog siv los tshem tawm cov pab pawg neeg tiv thaiv, thiab cov tau octapeptide yog acetylated nrog acetic anhydride los yog lwm yam acetylation reagents kom tau ctreotide. Cov tshuaj tiv thaiv tshwj xeeb thiab cov kauj ruam ua haujlwm yuav txawv nyob ntawm qhov kev sim thiab cov cuab yeej siv.
Kauj Ruam 3:
Purification thiab Crystallization: Purify cov ctreotide tau los ntawm txoj kev xws li recrystallization thiab chromatography los txhim kho nws cov purity thiab crystallinity. Txoj kev purification tshwj xeeb yog nyob ntawm cov khoom ntawm lub hom phiaj cov khoom thiab cov kev sim.
3. Cov yam ntxwv zoo:
Siv cov txheej txheem spectroscopic xws li nuclear magnetic resonance hydrogen spectroscopy thiab huab hwm coj spectrometry los ua tus yam ntxwv ntawm ctreotide tau los xyuas kom meej tias nws cov qauv zoo li qhov kev cia siab.
4. Kev soj ntsuam zoo:
Kev soj ntsuam zoo yog ua tiav ntawm cov ctreotide tau los ntawm cov txheej txheem xws li kev ntsuas qhov taw qhia melting thiab cov ntsiab lus tsom xam kom ntseeg tau tias nws qhov zoo thiab purity ua tau raws li qhov yuav tsum tau ua.
Kev sib npaug tshuaj
Vim muaj ntau cov kauj ruam thiab cov kev sim tshwj xeeb koom nrog hauv kev sib txuas ntawm ctreotide, nws nyuaj rau piav qhia tag nrho cov txheej txheem synthesis siv ib qho kev sib npaug tshuaj. Txawm li cas los xij, qee qhov kev sib npaug tshuaj rau cov kauj ruam tseem ceeb tuaj yeem muab tau raws li kev siv:
Kev sib npaug tshuaj rau kev sib txuas cov amino acids los tsim octapeptides: Cov kauj ruam no feem ntau yog tsim cov peptide bonds, uas tuaj yeem pab tau los ntawm kev siv cov tshuaj condensation xws li DCC (N, N '- dicyclohexylcarbamide) thiab HOBt (hydroxybenzotriazole). Qhov kev sib npaug tshuaj lom neeg tshwj xeeb yog raws li hauv qab no:
X-Y+Z → X-Y-Z+H2O
Ntawm lawv, X, Y, thiab Z sawv cev rau cov amino acid residues sib txawv, thiab "-" sawv cev rau kev tsim cov peptide bonds.
Cov tshuaj sib npaug rau tshem tawm cov pab pawg tiv thaiv thiab acetylation: Cov kauj ruam no feem ntau yog siv cov acids uas muaj zog los yog cov hauv paus tshem tawm cov pab pawg tiv thaiv, tom qab ntawd acetylation cov tshuaj tiv thaiv nrog acetic anhydride lossis lwm yam acetylation reagents. Qhov kev sib npaug tshuaj lom neeg tshwj xeeb yog raws li hauv qab no:
X-Y-Z+CH3COOH → X-Y-Z-CH3COOH+H2O
Ntawm lawv, X-Y-Z sawv cev rau octapeptide yam tsis tau tshem tawm pawg tiv thaiv, thiab "- CH3CO -" sawv cev rau pawg acetyl.
Cov lus nug nquag
Ctreotide siv rau dab tsi?
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Kev piav qhia. Kev txhaj tshuaj Octreotide yog siv los kho mob raws plab thiab lwm yam tsos mob uas tshwm sim nrog qee yam mob plab hnyuv (xws li, vasoactive plab hnyuv peptide hlav los yog VIPomas) lossis cov qog nqaij hlav qog nqaij hlav (cov qog nqaij hlav uas twb kis tau hauv lub cev lawm).
Vim li cas octreotode siv hauv GI los ntshav?
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Ntawm qhov kev txaus siab tshwj xeeb, octreotide nres GI hemorrhage los ntawm nws cov txheej txheem ntawm kev txo cov ntshav mucosal mus rau GI system thiab inhibiting acid thiab pepsin secretion, uas tiv thaiv kev daws teeb meem ntawm cov hlab ntsha ntawm qhov chaw los ntshav.
Puas yog ctreotide chemotherapy?
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Puas yog Sandostatin yog ib hom tshuaj khomob? Tsis yog, nws tsis yog ib hom tshuaj khomob, tab sis yog cov tshuaj hormones hluavtaws, zoo ib yam li cov tshuaj hormones uas tshwm sim hu ua somatostatin thiab siv los kho cov tsos mob (dej raws plab lossis dej ntws tawm) ntawm cov qog carcinoid thiab vasoactive plab hnyuv peptide hlav.
Koj tswj hwm octreotode acetate li cas?
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Octreotide los ua ib qho tam sim no - tso kua (kua) rau kev txhaj tshuajtxhaj tshuaj subcutaneously (nyob rau hauv daim tawv nqaij) los yog intravenously (rau hauv cov hlab ntsha)Octreotide kuj tuaj raws li qhov ntev - kev txhaj tshuaj kom txhaj rau hauv cov leeg pob tw los ntawm kws kho mob lossis tus kws saib xyuas neeg mob.
Puas yog octreotide yog tshuaj uas pheej hmoo siab?
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Octreotide tuaj yeem ua rau muaj teeb meem hauv plawv lossis lub plawv dhia, uas tuaj yeem ua rau lub neej - hem.Koj qhov kev pheej hmoo rau cov teeb meem no siab dua yog tias koj twb muaj teeb meem plawv lossis noj tshuaj uas tuaj yeem hloov koj lub plawv dhia thiab lub plawv dhia, xws li beta-blockers.
octreotide ua haujlwm sai npaum li cas?
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Octreotide pib ua haujlwmhauv ib teevTom qab txhaj tshuaj subcutaneous los kho hyperinsulinemia.
Cim npe nrov: octreotide acetate hmoov cas 83150-76-9, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom