Lanreotide hmoovyog cov tshuaj peptide nrog cov tshuaj npe N - [(1S) -1- [(2S, 3R) -3- (1-Carboxy-2-phenylethyl) -2-methyloxiran-2-yl] methyl] -3- (phenylmethod) propyl] - D tryptophanamide. Cov mis mos molecular yog C38H48N4O7S, CAS 108736-35-2, thiab qhov hnyav molecular yog 680.86. Nws yog xim dawb rau greyish dawb hmoov, tsw tsw. Solubility nyob rau hauv dej yog tsawg, tab sis nws muaj zoo solubility nyob rau hauv cov organic solvents xws li methanol thiab ethanol. Nws yuav tsum muaj ntau yam tshuaj tiv thaiv, suav nrog kev tiv thaiv, kev tiv thaiv, kev sib xyaw ua ke, thiab lwm yam tshuaj tiv thaiv. Thaum lub sij hawm synthesis, nws yuav tsum nruj me ntsis tswj cov tshuaj tiv thaiv tej yam kev mob, xws li kub, pH nqi, tshuaj tiv thaiv lub sij hawm, thiab lwm yam., kom ntseeg tau lub purity thiab tawm los ntawm cov khoom kawg. Nws yog ib qho kev loj hlob hormone analogue nrog ntau yam kev siv, ua lub luag haujlwm tseem ceeb hauv kev kho cov kab mob xws li acromegaly, carcinoid syndrome, pancreatic endocrine qog, kab mob gastroesophageal reflux, thiab pancreatic cystic fibrosis. Thaum siv lalotudine, nws yog ib qho tseem ceeb uas yuav tsum tau ua raws li tus kws kho mob cov lus qhia thiab tau txais kev saib xyuas tsis tu ncua kom ntseeg tau tias cov tshuaj muaj txiaj ntsig thiab kev nyab xeeb ntawm cov tshuaj. Thov nco ntsoov tias cov khoom tsim los ntawm Shaanxi BLOOM Tech Co., Ltd. yog cov tshuaj tseem ceeb thiab siv tsis tau rau kev kho mob.
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Customized Bottle Caps Thiab Corks:
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Tshuaj Formula |
C54H69N11O10S2 |
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Exact Mass |
1095 |
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Molecular Luj |
1096 |
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m/z |
1095 (100.0%), 1096 (58.4%), 1097 (16.7%), 1097 (9.0%), 1098 (5.3%), 1096 (4.1%), 1098 (3.1%), 1097 (2.4%), 1097 (2.1%), 1096 (1.6%), 1099 (1.5%), 1098 (1.2%) |
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Elemental Analysis |
C, 59.16; H, 6.34; N, 14.05; O, 14.59; S, 5.85 |
Lanrelin yog ib qho kev sib txuas ntawm kev loj hlob hormone inhibitor analogue, uas ua rau muaj kev cuam tshuam rau ntau yam tshuaj hormones, suav nrog kev loj hlob hormone, thyroid stimulating hormone (TSH), insulin, thiab glucagon. Lanrelin zoo ib yam li kev loj hlob hormone inhibin thiab ua los ntawm receptors. Nws muaj affinity ntau dua rau peripheral somatostatin receptors, kev ua haujlwm zoo sib xws, thiab tsis muaj kev sib raug zoo rau lub hauv nruab nrab paj hlwb. Txawm hais tias kev loj hlob hormone inhibin decomposes nyob rau hauv lub cev li ntawm ob peb feeb, lub sij hawm attenuation ntawm Lanrelin yog ntev dua, ua rau cov nyhuv ntev dua.
Lanreotide hmoovyog ib qho kev sib xyaw ua ke ntawm somatostatin analogue nrog kev siv dav hauv kev kho mob, feem ntau yog siv rau kev kho mob ntawm ntau yam kab mob endocrine thiab qog.
1. Kev kho mob ntawm acromegaly
Acromegaly yog ib yam kab mob tsis tshua muaj tshwm sim los ntawm kev tso tawm ntau dhau ntawm cov tshuaj hormones loj hlob (GH) los ntawm cov qog pituitary anterior. Cov neeg mob feem ntau ntsib cov kev hloov pauv ntawm cov qauv thiab cov kab mob endocrine metabolic vim qhov tso tawm ntau dhau ntawm GH thiab insulin-zoo li kev loj hlob zoo-1 (IGF-1), uas cuam tshuam rau lawv lub neej zoo thiab kev ua neej. Lanrui peptide, raws li ib tug somatostatin analogue, muaj peev xwm inhibit GH secretion, yog li txhim kho cov neeg mob cov tsos mob thiab zoo ntawm lub neej.
Lanrui peptide yog dav siv hauv kev kho mob ntawm acromegaly. Rau cov neeg mob uas muaj acromegaly nquag, suav nrog cov neeg uas tsis tau mus txog qib GH li qub tom qab kev phais pituitary GH qog, thiab cov neeg uas tseem tsis tau ua tiav cov txiaj ntsig kho mob txaus tom qab kev kho hluav taws xob sab nraud pituitary tab sis tseem muaj qib GH qib siab, lanrelitide yog cov tshuaj kho tau zoo. Nws tuaj yeem txo cov tsos mob xws li mob taub hau, tawm hws ntau dhau, qaug zog, mob pob qij txha, thiab lwm yam hauv cov neeg mob los ntawm inhibiting GH secretion thiab txo IGF-1 qib.
Cushing's syndrome yog ib qho kev kho mob uas tshwm sim los ntawm qhov ntev - lub sij hawm ntau dhau ntawm kev tso tawm ntawm glucocorticoids los ntawm adrenal cortex vim muaj ntau yam laj thawj, tseem hu ua endogenous Cushing's syndrome. Cov neeg mob feem ntau ntsib cov tsos mob xws li kev rog hauv nruab nrab, lub ntsej muag puv hli, zoo li muaj ntau cov ntshav, kab ntshav, thiab ntshav siab. Lanrui peptide kuj tseem muaj qee qhov txiaj ntsig ntawm kev kho mob ntawm Cushing's syndrome.
Lanrui peptide tuaj yeem tswj tus mob ntawm cov neeg mob Cushing's syndrome los ntawm inhibiting qhov tso tawm ntawm adrenocorticotropic hormone (ACTH). Rau cov neeg mob uas muaj Cushing's syndrome, kev siv lanreotide tuaj yeem txo cov tsos mob tsis zoo xws li kub siab, rog rog, thiab txhim kho lawv lub neej zoo.
Neuroendocrine hlav yog ib hom qog uas tshwm sim los ntawm cov hlwb neuroendocrine, nrog rau cov qog nqaij hlav carcinoid, pancreatic neuroendocrine qog, thiab lwm yam. Cov qog no feem ntau zais ntau yam tshuaj hormones thiab bioactive tshuaj, ua rau muaj cov tsos mob tshwm sim hauv cov neeg mob. Lanrui peptide kuj tseem muaj cov txiaj ntsig tseem ceeb hauv kev kho cov qog neuroendocrine.
Rau cov neeg mob uas muaj kab mob hauv plab hnyuv neuroendocrine thiab carcinoid syndrome, lanrelitide tuaj yeem txo cov tsos mob xws li raws plab, dej ntws tawm, electrolyte imbalance, thiab exudative polymorphic pob. Lub caij no, Lanrui peptide kuj tuaj yeem siv rau kev kho mob ntawm cov qib siab, zoo sib txawv lossis sib txawv me ntsis, tsis ua haujlwm, thiab kev loj hlob hormone receptor zoo neuroendocrine hlav, xws li kab mob plab thiab pancreatic neuroendocrine hlav.
Mob qog noj ntshav mis yog ib qho mob qog nqaij hlav ntau tshaj plaws hauv cov poj niam, uas ua rau muaj kev hem thawj rau poj niam lub neej thiab kev noj qab haus huv. Lanruitide kuj tseem muaj qee qhov txiaj ntsig hauv kev kho mob qog noj ntshav mis. Txawm hais tias Lanruitide tsis yog cov tshuaj kho mob tseem ceeb rau mob qog noj ntshav, nws tuaj yeem siv los ua kev kho mob hauv qee kis los pab cov neeg mob txo cov tsos mob thiab txhim kho lawv lub neej zoo.
Piv txwv li, rau cov neeg mob postmenopausal nrog mob qog noj ntshav mis, Lanruitide tuaj yeem xaiv khi rau gonadotropin tso cov tshuaj hormone receptor, thaiv nws txoj kev xaim hluav taws xob nrog G-protein coupled receptor, txo intracellular calcium concentration, inhibit cell division, induce qog cell apoptosis, thiab yog li ua lub luag haujlwm tiv thaiv - qog.
5. Lwm yam kev siv
(1) Kev kho mob qog noj ntshav ntawm qhov quav: Lanrui peptide kuj muaj qee yam kev siv nyiaj hauv kev kho mob qog noj ntshav ntawm qhov quav. Txawm hais tias txoj kev kho mob tseem ceeb rau kev mob qog noj ntshav yog kev phais thiab kws khomob, lanrelitide tuaj yeem siv los ua kev kho mob ntxiv los pab cov neeg mob txo cov tsos mob thiab txhim kho lawv lub neej zoo.
(2) Kev kho mob qog noj ntshav prostate: Lanrui peptide tuaj yeem cuam tshuam prostate cell proliferation zoo, yog li ua tiav lub hom phiaj ntawm kev txo qis prostate ntim. Yog li ntawd, nws tuaj yeem siv los ua kev kho mob ntxiv rau kev mob qog noj ntshav prostate los pab cov neeg mob tswj qhov kev loj hlob ntawm tus kab mob.
(3) Kev tswj qhov mob: Lanrui peptide tuaj yeem txo qis kev ua haujlwm neuronal thiab txo qhov mob los ntawm kev thaiv cov haujlwm ntawm cov paj hlwb. Qhov no tej zaum yuav yog ib qho kev kho mob zoo rau qee cov neeg mob uas nws qhov mob tsis yooj yim tswj tau.
(4) Kev txhim kho cov tsos mob ntawm plab hnyuv: Lanrui peptide muaj cov txiaj ntsig ntawm kev txhawb nqa lub plab zom mov, txhim kho plab zom mov thiab nqus dej, thiab pab txhim kho cov tsos mob tsis xis nyob xws li poob qab los noj mov thiab tsam plab. Qhov no tej zaum yuav yog ib qho kev kho mob zoo rau qee cov neeg mob uas muaj kab mob digestive.
Amino acid tiv thaiv:Tiv thaiv kom raug cov amino acids uas yuav tsum tau muaj kom tsis txhob muaj kev cuam tshuam tsis tsim nyog thaum lub sij hawm sib xyaw ua ke - theem. Cov amino acid tiv thaiv pawg muaj xws li 9-fluoromethyl chloride (Fmoc), p-methoxybenzyl ester (Pbf), thiab lwm yam. Cov pab pawg tiv thaiv no tuaj yeem thaiv qee qhov chaw tshuaj tiv thaiv ntawm cov amino acids thaum lub sij hawm cov txheej txheem tshuaj tiv thaiv, yog li tswj qhov tshwj xeeb ntawm cov tshuaj tiv thaiv.
Solid Phase Synthesis:Raws li cov amino acid sib lawv liag ntawm Lanrelin, cov amino acids tiv thaiv tau txuas mus rau cov resin los ntawm cov khoom sib xyaw ua ke -theem synthesis. Nyob rau hauv cov txheej txheem no, nws yog ib qho tsim nyog los xaiv cov kev sib txuas uas tsim nyog thiab kev sib txuas ua ke kom ntseeg tau tias txhua tus amino acid tuaj yeem txuas mus rau cov amino acid yav dhau los. Cov kab mob sib txuas muaj xws li dichloromethane, dichloroquinoline, thiab lwm yam.
Cov txheej txheem sib xyaw ua ke los ntawm pyrolysis:Tom qab ua tiav, lub synthesized peptde yuav tsum tau cleaved los ntawm resin. Cov txheej txheem no feem ntau yog siv cov kua qaub uas muaj zog lossis muaj zog hauv paus daws kom tawg kev sib txuas ntawm cov amino acids thiab cob. Tom qab pyrolysis, peptde yuav tsum tau ntxuav kom huv si kom tshem tawm impurities thiab unreacted amino acids.
Linear peptide cyclization:Tom qab tau txais cov kab peptdes, lawv yuav tsum tau cyclized nrog cov oxidants tshwj xeeb kom tau txais cov qauv cyclic ntawm Lanrelin. Cov oxidants feem ntau muaj xws li iodine oxidants, hydrogen peroxide oxidants, thiab lwm yam. Cov txheej txheem no yuav tsum tau ua raws li cov pH tshwj xeeb thiab qhov kub thiab txias kom ntseeg tau tias kev ua haujlwm ntawm cyclization thiab kev ruaj ntseg ntawm cov khoom.
Purification thiab crystallization:Tom qab cyclization, peptde yuav tsum tau ua kom huv ntxiv kom tau txais siab -purity xiav ray peptde. Cov txheej txheem purification muaj xws li gel pom, ion pauv, thiab lwm yam. Crystallization yog ib qho tseem ceeb hauv kev txhim kho cov khoom purity thiab stability. Los ntawm kev tswj cov crystallization tej yam kev mob xws li kub, pH, concentration, thiab lwm yam., siab -zoo xiav peptde crystals yuav tau.
Pharmacokinetics
Kev nqus kinetics ntawm Lanrui peptide nyob rau hauv cov neeg ua haujlwm noj qab haus huv los ntawm kev txhaj tshuaj intramuscular ntawm cov tshuaj yog tus cwj pwm los ntawm kev tso tawm sai hauv thawj theem, uas yog kev tso tawm ntawm peptides khi rau saum npoo ntawm cov khoom, ua raws li qeeb qeeb hauv theem thib ob ntawm kev tso tawm. Thawj plasma ncov (Cmax 1: 6.8 ± 3.8 μ g / L) yog nyob ntawm 1.4 ± 0.8 teev, thiab lub ncov thib ob (Cmax 2: 2.5 ± 0.9 μ g / L) yog ntawm 1.9 ± 1.8 hnub, nrog rau qhov bioavailability ntawm 4.61%. Lub sij hawm khaws cia nruab nrab yog 8.0 ± 1.0 hnub, thiab qhov chaw ib nrab -lub neej yog 5.2 ± 2.5 hnub, uas ua pov thawj qhov kev txhawb nqa - tso tawm cov yam ntxwv ntawm cov tshuaj. Rau cov neeg mob acromegaly, muaj qhov txo qis hauv kev loj hlob hormone thiab IGF-1 qib tsawg kawg yog 14 hnub tom qab txhaj tshuaj ib zaug. Rov muab tshuaj rau ob peb lub hlis yam tsis muaj tshuaj ntxiv.
Cov lus nug nquag
Cov tshuaj lanreotide ua dab tsi?
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Kev txhaj tshuaj Lanreotide yog siv los kho cov neeg uas muaj acromegaly (qhov xwm txheej uas lub cev tsim cov tshuaj hormones loj hlob ntau dhau, ua rau lub ntsej muag loj, ob txhais taw, thiab lub ntsej muag; mob pob qij txha; thiab lwm yam tsos mob) uas tsis ua tiav, lossis kho tsis tau nrog kev phais lossis hluav taws xob.
Puas yog lanreotide thiab octreotide tib yam?
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Muaj qhov sib txawv me ntsis hauv FDA pom zoo: octreotide (Sandostatin) tau pom zoo rau cov tsos mob ntawm carcinoid/VIPoma syndrome thiab Lanreotide (Somatuline) tau pom zoo rau kev tswj cov qog.
Koj yuav tsum tau noj dab tsi thaum noj lanreotide?
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Tsis tas li ntawd, kev hloov kev noj haus yuav pab tau. Zam tej yam uas yuav ua rau cov tsos mob hnyav dua, xws lihnyav los yog greasy / fatty, ntsim, los yog acidic zaub mov (txiv qaub, txiv lws suav, txiv kab ntxwv). Sim tshuaj antacids (xws li mis nyuj ntawm magnesia, calcium ntsiav tshuaj xws li Tums), ntsev, los yog Ginger ale kom txo cov tsos mob.
Koj tuaj yeem nyob ntev npaum li cas ntawm lanreotide?
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Yog tias koj muaj lanreotide los tswj kev loj hlob ntawm koj NET, koj txuas ntxiv qhov no rautsuav nws ua haujlwm, thiab cov kev mob tshwm sim tsis zoo heev.
Cim npe nrov: Lanreotide hmoov CAS 108736-35-2, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom