Etelcalcetide cas 1262780-97-1

Licalcetideyog dawb lossis yuav luag dawb crystalline hmoov, qee zaum kuj yog lub teeb daj xim. Nws feem ntau tsis muaj ntxhiab thiab soluble hauv dej. Tshuaj mis siv tshuaj yog c26h27n5o2, nrog tus txheeb ze ua ke hnyav ntawm 445.531 g / mol. Nws yog cov tshuaj antidepresspressionant uas yog xaiv cov serotonin ruptor (SSRI) thiab ib feem ntawm cov serotonin 1a receptor. Nws muaj kev sib hloov kho qhov muag, nrog kev sib hloov lub kaum sab xis ntawm {{}} degree rau {{8} degree (10mg / ml, hauv dej). Nws yog chairal molecule uas yuav tsim cov enantiomers sib txawv thaum tshuaj lom neeg. Vim tias muaj cov enantiomers, tej zaum yuav muaj qhov sib txawv ntawm lawv cov khoom siv kho tshiab thiab lwm yam kho tshiab. Qhov kev ua kom muaj qhov ua rau muaj kev nqus tau cov kab ke peaks, thiab kev ncab kev co nqus lub ncov ntawm NH tuaj yeem pom ntawm kwv yees li 3400 cm {{}; Pom kev co nqus nqus nqus tau lub ncov ntawm CH3 tuaj yeem pom ntawm kwv yees li 2920 cm -1; Kev ncab kev co nqus nqus nqus tau lub ncov ntawm cov co tuaj yeem pom ntawm kwv yees li 1650 cm -1; Ib qho kev ncab kev vibration nqus lub ncov ntawm lub nplhaib uas muaj ntxhiab tuaj yeem pom ntawm kwv yees li 1500 cm {{18}.

Licalcetideyog ib qho ntawm qhov ncauj dipeptidas 4 (DPP -4}}) Inhibitor, tsuas yog siv los kho hom ntshav qab zib hom 2. Raws li hom tshiab ntawm cov tshuaj tiv thaiv kab mob ntshav qab zib, nws muaj ntau lub zog, uas yog qhov tseem ceeb los txhim kho cov ntshav qab zib tswj thiab lub neej zoo ntawm cov neeg mob ntshav qab zib.

1. Txo cov ntshav qab zib ntshav

Lub luag haujlwm tseem ceeb yog kom muaj cov ntshav qab zib qis dua. Nws txo qhov kev cuam tshuam ntawm genucagon zoo li peptide -1 (gip} (gip} (gip}) GLP {{{}}} thiab gip tuaj yeem txhawb nqa cov tso pa insulin, inhibit tso tawm glucagon, thiab yog li muaj cov ntshav qab zib qis. Cov nyhuv ntawm Veracatide yog qhov muaj txiaj ntsig los txhim kho cov ntshav qab zib tswj cov ntshav qab zib thiab txo qhov tshwm sim ntawm cov teeb meem.

2. Txhim Kho Insulin Kuj

Insulin tsis kam yog ib qho ntawm cov yam ntxwv tseem ceeb ntawm hom 2 yam mob ntshav qab zib. Nws cov tshuaj kho cov insulin tsis kam los ntawm nce insulin rhiab heev. Nws tuaj yeem txhawb nqa lub Uptake thiab siv cov tshuaj insulin los ntawm adipocytes thiab cov leeg nqaij, txhim kho cov tshuaj insulin, thiab yog li txhim kho lub cev rhiab rau cov tshuaj insulin. Cov nyhuv no yuav pab txo cov ntshav qab zib thiab txo qhov xav tau rau cov tshuaj insulin rau cov neeg mob ntshav qab zib.

3. Txhawb kev txhim kho ntawm tes ntawm tes thiab kev rov ua haujlwm zoo

Nws tseem muaj txoj haujlwm ntawm kev txhawb nqa pancreatic islets lub luag haujlwm ntawm kev tsim kho ntawm tes thiab kev ua haujlwm rov ua haujlwm. Los ntawm inhibiting qhov kev ua ntawm DPP -4 Enzyme tuaj yeem ua tiav cov ntshav qab zib yog kev tiv thaiv oxidative, txhawb nqa lub hlwb. Tsis tas li ntawd, nws kuj tuaj yeem nce cov synthesis thiab kev zais ntawm cov insulin, txhim kho kev ua haujlwm ntawm cov hlwb. Cov teebmeem no muaj txiaj ntsig zoo los txhim kho Islet ua haujlwm ntawm cov neeg mob ntshav qab zib thiab nce qib ntawm insulin kev zais cia.

4. Txo qhov hnyav thiab muaj roj zuj zus

Nws kuj muaj cov nyhuv ntawm kev txo qhov hnyav thiab roj zuj zus. Nws tuaj yeem txo lub qab los noj mov thiab zaub mov noj kom tsawg, thiab qis zog. Nyob rau tib lub sijhawm, Veracalide tseem tuaj yeem txhawb kev puas tsuaj thiab metabolism ntawm cov rog, txo cov rog hauv lub cev. Cov nyhuv no tuaj yeem pab txhim kho kev rog ntawm cov neeg mob ntshav qab zib thiab txo qhov kev pheej hmoo ntawm cov kab mob plawv thiab lwm yam teeb meem.

5. Txhim Kho Cov Kab Mob Lipid Metabolism

Nws tseem tuaj yeem txhim kho cov roj av lipid lipid thiab txo cov ntshav lipid. Nws tuaj yeem nce cov synthesis thiab zais ntawm cov lipoprotein high-density lipoprotein (HDL), thiab txo cov lipoprotein tsawg (LDL) thiab tag nrho cov cholesterol). Ib qho ntxiv, nws tseem tuaj yeem txwv cov cuab yeej thiab kev sib txuam ntawm cov triglycerides, thiab txo qib ntawm triglycerides hauv ntshav. Cov teebmeem no pab txo qhov kev pheej hmoo ntawm cov kab mob plawv hauv cov neeg mob ntshav qab zib.

6. Kev tiv thaiv cov hlab plawv

Nws tseem muaj cov nyhuv tiv thaiv ntawm cov hlab plawv. Nws tuaj yeem txo cov ntshav siab, txo qhov tshwm sim ntawm cov kab mob plawv plawv xws li lub siab hypertroh thiab myocardial puas. Tsis tas li ntawd, nws tseem tuaj yeem txwv qhov mob thiab oxidatatory kev tawm tsam ntawm cov hlwb endothelial, tiv thaiv kev noj qab haus huv thiab kev ntseeg ntawm cov hlab ntshav. Cov teebmeem no pab txo txoj kev pheej hmoo ntawm cov kab mob plawv hauv cov neeg mob ntshav qab zib thiab txhim kho lub neej zoo.

7. Txhim Kho Kev Ncaj Ncees

Cov kev tshawb fawb tsis ntev los no tau pom tias nws tseem muaj qhov cuam tshuam ntawm kev txhim kho kev ua haujlwm. Nws tuaj yeem nce cov ntsiab lus thiab kev ua haujlwm ntawm cov neurotransmitters hauv lub hlwb, xws li acetylcholine thiab dopamyine, thiab txhim kho qhov kev sib kis tau zoo thiab cov ntaub ntawv sib kis tau zoo ntawm neurons. Tsis tas li ntawd, nws tseem tuaj yeem txwv tsis pub o thiab oxidative kev nyuaj siab nyob rau hauv lub hlwb, tiv thaiv kev noj qab haus huv thiab muaj sia nyob ntawm neurons. Cov teebmeem no yog txiaj ntsig los txhim kho kev txawj ntse ntawm cov neeg mob ntshav qab zib thiab txhim kho lub neej zoo.

8. Txhim Kho Lub Neej Zoo

Hauv cov ntsiab lus, los ntawm kev txo cov ntshav qab zib, txhim kho cov kev txhim kho ntawm tes, kev ua kom zoo dua qub muab kev kho mob ntawm tes, thiab kev ua haujlwm zoo rau cov neeg mob ntshav qab zib. Kev thev ntawm cov kev tswj hwm cov ntshav qab zib thiab kev pheej hmoo ntawm cov neeg mob ntshav qab zib, txo cov kev pheej hmoo ntawm tus nqi ntshav qab zib thiab kev muaj sia nyob ntawm tus neeg mob. Yog li ntawd, Veracatide muaj cov nqi kho mob tseem ceeb thiab daim ntawv thov cia siab hauv kev kho mob ntshav qab zib.

LicalcetideYog dipeptidyl peptidase 4 (DPP -4) Inhibitor, uas yog siv los kho hom ntshav qab zib hom 2. Nws cov synthesis cuam tshuam ntau cov kauj ruam, thiab cov hauv qab no yuav muab cov lus qhia ntxaws ntxaws rau nws cov kev ntsuas hluav taws xob synthesis thiab coj cov tshuaj sib luag ncaj ncees.

Cov kauj ruam synthesis:

1. Ua kom cov amino acids

Firstly, nws yog ib qhov tsim nyog los xaiv cov amino acids uas tsim nyog rau kev ua kom muaj zog. Cov txheej txheem ua kom muaj zog yog qhib cov pab pawg carboxyl siv n-hydroxysuccinimide (NHS) thiab n '- DICYCLOHXYXYRCARIIMIDE (DCC).

Tshuaj lom neeg tshuaj lom neeg (siv L-Alanine ua piv txwv):

C₃H₇Tsis muaj₂+C₄H₅Tsis muaj₃+C₁₃H₂₂N₂ → C₃H₇Tsis muaj₂NHS + C₁₃H₂₄N₂O

Ntawm lawv, DCU yog n, n '- Dicyclohexylurea, uas yog breproduct ntawm cov tshuaj tiv thaiv.

2. Cov tshuaj tiv thaiv

Cov amino acid undergoes ib cov tshuaj tiv thaiv hws nrog cov amino pab pawg ntawm cov amino acid tom ntej no los ua peptide daim ntawv cog lus. Cov kauj ruam no feem ntau tau nqa tawm hauv cov xwm txheej alkaline, xws li siv Triethylamine ua lub hauv paus.

Tshuaj lom neeg mob tshuaj (siv L-Alanine thiab L-Leucine ua piv txwv):

C₃H₇Tsis muaj₂-Nws + c₆H₁₃Tsis muaj₂+C₆H₁₅N → C₃H₇Tsis muaj₂-L-C₆H₁₃Tsis muaj₂+H₂O + NHS - Triethylamine ntsev

3. Txuas ntawm peptide saws

Los ntawm kev rov ua cov tshuaj tiv thaiv hws, maj mam txuas cov amino acids uas yuav tsum tau ua rau peptide saw kom txog thaum ua ntu zus ntawm Veracalide tau txais.

4. Cyclization Revere

VeracapEctide Molecules muaj cov qauv kev sib txawv uas yuav tsum tau tsim los ntawm kev sib cav sib ceg. Qhov no feem ntau cuam tshuam nrog kev tawm tsam ntawm ib sab xib saw pawg thiab lwm pab pawg ntawm peptide saw.

Tshuaj lom neeg tshuaj lom neeg (siv cov thooj yooj yim ntawm Veracalide ua piv txwv):

H₂N peptide saw co-r 1+ peptide saw co-r2 → [h₂N peptide saw co-r1] - peptide saw co-r {{}} h₂O

R1 thiab R2 sawv cev cov pab pawg sib txawv ntawm peptide saw, tsim cov qauv cyclic los ntawm cov tshuaj tiv thaiv.

5. Kev ua kom huv thiab crystallization

Tom qab ua tiav kev sib cav sib cav sib ceg, cov khoom yuav tsum ua kom huv thiab crystallized kom tau txais cov veracalide high-purity veracalide. Qhov no feem ntau yog koom nrog cov kauj ruam xws li kem chromatography, nyias-txheej chromatography, thiab recrystallization.

Txoj kev txhim kho kev cia siab ntawmLicalcetideYog qhov dav dav heev, tsuas yog raws nws qhov kev cuam tshuam tseem ceeb thiab kev sib txawv ntawm kev nqis tes ua hauv kev kho mob. Cov hauv qab no yog cov ncauj lus kom ntxaws ntxaws ntawm nws txoj kev txhim kho tom ntej:

Cim npe nrov: Etelcalcetide Cas 1262780-97-1, cov chaw muag khoom, chaw tsim khoom, Hoobkas, lag luam, yuav, nqe, loj, rau muag