cov khoom siv

EUK-134 (81065-76-1)

EUK 134 yog cov khoom siv hluavtaws manganese-porphyrin uas tau sau tseg los ua cov tshuaj tua kab rau cov kab mob oxidative xws li hydrogen peroxide, peroxynitrite thiab superoxide. Cov sib xyaw no yog salen-manganese complex uas tau hloov kho kom nws cov catalase ua haujlwm thaum khaws SOD cov haujlwm.

Wisepowder muaj peev xwm tsim tau thiab muab khoom ntau. Txhua qhov kev tsim khoom raws li cGMP thiab kev tswj hwm nruj, tag nrho cov ntaub ntawv xeem thiab cov qauv muaj.
Qeb:

EUK-134 hmoov Base Qhia

lub npe  UA-134
CAS 81065-76-1
purity 98%
Tshuaj lub npe chloro [[2,2 ′-[1,2-ethanediylbis [(nitrilo-κN) methylidyne]]] bis [6-methoxyphenolato-κO]]]-manganese
Synonyms EUK 134; SALEN-MN; Salen-Mn-Cl; SALEN-MN/EUK-134; SALEN-MN USP/EP/BP; EUK 134, SOD/catalase mimetic; Manganese (salen-3,3′-diMethoxy) chloride ; ETHYLBISIMINOMETHYLGUAIACOL MANGANESE CHLORIDE; chloro (bis (3,3′di-methoxysalicylidene) ethylenediamine) manganese; EUK 134, SOD/catalase mimetic, Ethylbisiminomethylguaiacol manganese chloride
molecular Formula C18H18ClMnN2O4
molecular Nyhav 416.7
melting Point > 300 ° C.
InChI Qhov Tseem Ceeb YUZJJFWCXJDFOQ-GAMUHHASSA-K
daim ntawv Khoom
tsos Tsaus xim av hmoov
Ib Sim Neej /
solubility Soluble hauv dej (0.2 mg/ml ntawm 25 ° C), PBS pH 7.2, ethanol, DMSO, thiab DMF.
cia mob Khw tom-20 ° C
Daim ntawv thov EUK-134 tau siv los ua tshuaj tiv thaiv kab mob.

EUK-134 tau siv los txiav txim siab cov txheej txheem hauv qab hypoxia-inducible factor-1α (HIF-1α) kev ruaj khov hauv tib neeg aortic endothelial cells (HAECs).

Kuaj Cov Ntaub Ntawv Qhov

 

UA-134 81065-76-1 General hauj lwm

Salen manganese complex nrog superoxide dismutase (SOD) thiab catalase mimetic yam ntxwv. EUK134 nthuav tawm cov haujlwm muaj zog tiv thaiv kab mob antioxidant, thiab txwv tsis pub tsim β-amyloid thiab cuam tshuam txog amyloid fibril (IAPP). Cov cuab yeej siv tshuaj muaj txiaj ntsig zoo rau kev txhim kho cov tshuaj sib txuas tshiab rau kev kho mob Alzheimer's thiab Parkinson's disease thiab hom 2 mob ntshav qab zib.

Hauv SK-N-MC cells, EUK134 tiv thaiv cov hlwb neuronal tiv thaiv H2O2 kev lom los ntawm kev ua kom tsis txhob muaj kev nyuab siab los ntawm kev txwv tsis pub MAPK txoj hauv kev, thiab tseem ua rau txo qis kev qhia ntawm cov pro-apoptotic genes p53 thiab Bax ntxiv rau txhim kho kev qhia ntawm anti-apoptotic Bcl- 2gen ua. Kev kho ua ntej nrog EUK-134 (10 μM) tau muaj txiaj ntsig zoo hauv kev tiv thaiv kev hloov pauv ntshav siab hauv H9C2 hlwb, txo qis kev ntxhov siab oxidative, thiab tiv thaiv kev hloov pauv hauv lub cev. EUK-134 kev kho mob txhim kho cov txheej txheem oxidative ntawm mitochondria thiab thim rov qab hypertrophy-txo qis ntawm mitochondrial membrane muaj peev xwm. Kev txhawb ntxiv nrog EUK-134 yog li ntawd tau txheeb pom tias yog txoj hauv kev tshiab los txo qis kev mob plawv thiab ua rau muaj kev txhim kho EUK-134 ua tus neeg saib xyuas kev kho mob hauv tib neeg kab mob plawv.

 

UA-134 81065-76-1 Mechanism Of Action

Tib neeg haus cov zaub mov thiab dej txhua hnub, thauj lawv mus rau ntau yam ntaub so ntswg hauv lub cev los ntawm kev zom zaub mov thiab cov hlab ntshav, thiab tau hloov pauv hauv cov cell kom tso lub zog. Thaum lub sijhawm tag nrho cov txheej txheem zom zaub mov, ntau "ROS (hom pa oxygen)" yuav tsim tawm, suav nrog: O2-, H2O2 thiab HO2-, -OH, thiab lwm yam. , ua rau cell apoptosis thiab txawm tias necrosis.

Ob qhov tseem ceeb tiv thaiv kab mob tiv thaiv kab mob hauv tib neeg lub cev yog: superoxide dismutase (SOD) thiab catalase (CAT). Ob lub Cheebtsam no ua haujlwm sib koom ua ke txhawm rau hloov pauv "ROS (Reactive Oxygen Cluster)" uas tsim tawm hauv cov txheej txheem zom zaub mov rau hauv dej thiab oxygen kom tswj tau lub cev li qub cov metabolism.

Vim tias qhov hnyav molecular hnyav ntawm SOD, nws nyuaj rau nkag mus rau hauv stratum corneum. Ib qho ntxiv, txawm tias SOD nkag rau ntawm daim tawv nqaij me me los ntawm cov qhov hws thiab cov qog hws, nws yooj yim hydrolyzed los ntawm cov protein thiab muaj kev ruaj ntseg tsis zoo thiab cov metabolism hauv sai hauv tib neeg lub cev. Cov yam ntxwv ntawm SOD tiv thaiv nws daim ntawv thov hauv tshuaj pleev ib ce. Yog li, "EUK-134" tau tsim los hloov daim ntawv thov SOD thiab CAT hauv cov tshuaj pleev ib ce.

 

UA-134 81065-76-1 Daim ntawv thov

Tiv thaiv DNA puas tsuaj

Kho DNA

Anti-inflammatory

tiv thaiv oxidation

Kev saib xyuas tshuaj pleev thaiv hnub, ntxiv kev saib xyuas uas cov khoom siv tshuaj pleev thaiv hnub tsis tuaj yeem saib xyuas

Anti-voos

Sib ntaus oxidative kev nyuaj siab

Kev tiv thaiv kev ntxhov siab

 

UA-134 81065-76-1 Tshawb nrhiav ntxiv

EUK 134 yog salen-manganese complex uas tau hloov kho kom nws cov catalase ua haujlwm thaum khaws SOD cov haujlwm. EUK 134 yog salen-manganese complex uas tau hloov kho kom nws cov catalase ua haujlwm thaum khaws SOD cov haujlwm. EUK 134 siv hydrogen peroxide nrog thawj qhov tshuaj tiv thaiv ntawm 234 /M/min hauv vitro.1 EUK 134 yog tiv thaiv hauv tus qauv mob hlab ntsha tawg, ua haujlwm nruab nrab ntawm cov hlab ntshav hlab ntshav. Ntawm 2.5 mg/kg, nas kho nrog EUK 134 pom tias txo qis infarct ntim ntau dua 80%. EUK 134 ntawm 10 mg/kg kuj tseem ua rau lub hlwb puas hauv cov nas tom qab kev tswj hwm ntawm kainic acid.2

 

UA-134 81065-76-1 reference

  1. J Pharmacol Exp Ther. 1998 Lub Ib Hlis; 284 (1): 215-21; Proc Natl Acad Sci Asmeskas A. 1999 Lub Yim Hli 17; 96 (17): 9897-902; PLoS ib. 2017 Lub Ob Hlis 2; 12 (2): e0169146; Mol Cell Biochem. 2016 Cuaj Hlis; 420 (1-2): 185-94.
  2. J. Ophoven li al. Salen-manganese complexes: cov cuab yeej siv tau zoo rau kev tshuaj xyuas ntawm intercellular ROS teeb tsa txoj hauv kev. Anticancer Res Cov. 2010 Kaum Hli; 30 (10): 3967-79.
  3. Failli li al. Ib qho tshiab manganese complex ua tau zoo raws li superoxide anion scavenger thiab kho tus neeg sawv cev tiv thaiv cell thiab cov nqaij mos oxidative raug mob. J Med Chem. 2009 Kaum Ib Hlis 26; 52 (22): 7273-83.
  4. Decraene li al. Cov khoom siv hluavtaws superoxide dismutase/catalase mimetic (EUK-134) txwv tsis pub cov membrane-puas-ua kom muaj zog ntawm mitogen-activated protein kinase pathways thiab txo p53 tsub zuj zuj ... J nqis peev Dermatol. 2004 Lub Ob Hlis; 122 (2): 484-91.

 

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