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EUK-134 (81065-76-1)

EUK 134 o se synthetic manganese-porphyrin complex lea na faʻamaonia e galue o se scavenger mo ituaiga oxidative pei o hydrogen peroxide, peroxynitrite ma superoxide. O lenei tuʻufaʻatasiga o se salen-manganese complex lea ua toe faʻaleleia e faʻatele ai ana gaioiga a o taofia pea le gaioiga a le SOD.

Wisepowder ei ai le gafatia e gaosia ma tuʻuina atu se aofaʻi tele. Gaosia uma i lalo o le cGMP tulaga ma faiga pulea lelei atoatoa, pepa uma suʻega ma faʻataʻitaʻiga avanoa.
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EUK-134 paʻu Faʻamatalaga Faʻavae

igoa  EUK-134
CAS 81065-76-1
Mama Atoatoa i Tulaga 98%
Igoa faʻapitoa 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
Faiga Faʻavae Molecular C18H18ClMnN2O4
Taumaʻa Masele 416.7
liusuavai Point > 300 ° C
InChI Key YUZJJFWCXJDFOQ-GAMUHHASSA-K
faiga malō
Faʻaaliga Pulu uliuli enaena
Afa o le Ola /
Solubility Soluble i le vai (0.2 mg / ml i le 25 ° C), PBS pH 7.2, ethanol, DMSO, ma DMF.
teuina o Meaai a Tuutuuga Teu i -20 ° C
talosaga EUK-134 sa faʻaaogaina o se vailaʻau e puipuia ai le tino.

EUK-134 na faʻaaogaina e fuafua ai le faʻavae o loʻo faʻavaeina ai le hypoxia-inducible factor-1α (HIF-1α) faʻamautuina i sela o tagata endothelial aortic (HAECs).

Pepa o suʻega iai

 

EUK-134 81065-76-1 Faamatalaga Aoao

O le salen manganese complex ma superoxide dismutase (SOD) ma catalase mimetic uiga. EUK134 faʻaalia gaioiga malosi o le antioxidant, ma taofia ai le fausiaina o le β-amyloid ma le amyloid fibril (IAPP). E aoga mea tau vailaʻau mo le atinaʻeina o vailaʻau fou mo le togafitia ole faʻamaʻi ole Alzheimer ma Parkinson male maʻi suka ituaiga 2.

I sela o le SK-N-MC, EUK134 puipuia sela o le neuronal faasaga i le oona o le H2O2 e ala i le faʻamalosia o le atuatuvale o le oxidative e ala i le taofiofia o le auala MAPK, ma faʻaiʻu ai foi i le faʻaititia o faʻaaliga apoptotic genes p53 ma Bax faʻapea foʻi ma faʻalautelega faʻaalia o anti-apoptotic Bcl- 2 gafa Pretreatment ma EUK-134 (10 μM) na aoga i le puipuia o hypertrophic suiga i sela H9C2, faʻaititia o le faʻamalosiʻau oxidative, ma le puipuia o metabolic sifi. EUK-134 togafitiga faʻaleleia le tulaga oxidative o mitochondria ma suia hypertrophy-faʻaosoina faʻaititia o mitochondrial membrane gafatia. O le faʻaopopoga ma le EUK-134 ua faʻailoa mai o se auala fou e faʻaosofia ai le fatu hypertrophy ma faʻaavanoaina avanoa mo le atinaʻeina o le EUK-134 o se vailaʻau e faʻatautaia ai togafitiga o tagata fatu fatu.

 

EUK-134 81065-76-1 Mfaiga Of Afaʻasologa

E 'aʻai e tagata meaʻai ma vai i aso uma, ave latou i tino eseese ole tino e ala ile digestive system ma le faʻagaioiga o totoga, ma e gaosia ile sela e faʻasaʻoloto ai le malosi. I le taimi atoa o le metabolism, o le tele o "ROS (reactive oxygen ituaiga)" o le a gaosia, e aofia ai: O2-, H2O2 ma HO2-, -OH, ma isi. , e tau atu i le apoptosis sela ma e oʻo lava i le nerosis.

O vaega taua e lua o le antioxidant i le tino o le tagata: superoxide dismutase (SOD) ma catalase (CAT). O vaega ia e lua e galulue vavalalata e faʻaliliu le "ROS (Reactive Oxygen Cluster)" gaosia i le metabolic process i le vai ma le okesene e faʻatumauina ai le masani ai o le tino.

Ona o le maualuga molemeta mamafa o le SOD, e faigata ona ulu i le stratum corneum. I se faʻaopopoga, tusa lava pe ulufale le SOD i le paʻu i se vaega laititi e ala i afu ma afu afu, e faigofie lava ona faʻamumuina e le polotini ma e leaga le mautu ma vave le metabolism i le tino o le tagata. O nei uiga o le SOD puipuia lona faʻaaogaina i mea teuteu. O le mea lea, "EUK-134" na atiaʻe e sui ai le faʻaaogaina o le SOD ma le CAT i le vaega teuteu foliga.

 

EUK-134 81065-76-1 talosaga

Puipui mai le faʻaleagaina ole DNA

Lipea DNA

Aneti-inflammatory

anti-oxidation

Tausiga o le sunscreen, faʻaopopo le tausiga e le mafai e le lautele o mea e faʻaaoga i le la

Aneti-ita

Tau i le faʻamama o le oxidative

Aneti-popole

 

EUK-134 81065-76-1 Tele suesuega

EUK 134 o se salen-manganese complex na suia e faʻatele ai lona gaioiga gaioiga ao taofia SOD gaioiga. EUK 134 o se salen-manganese complex na suia e faʻatele ai lona gaioiga gaioiga ao taofia SOD gaioiga. EUK 134 faʻaumatia hydrogen peroxide ma le amataga tali fua faatatau o 234 µM / min in vitro.1 EUK 134 o se puipuiga i se isumu taʻi faʻataʻitaʻiga, faʻaaogaina ogatotonu cerebral alatoto ligation. I le 2.5 mg / kg, o isumu na togafitia ile EUK 134 na faʻaititia ai le faʻaititia ole infarct volume e ova atu ile 80%. EUK 134 i le 10 mg / kg faʻapea foi ona matua faʻaitiitia ai le faʻaleagaina o faiʻai i isumu mulimuli ane i le faʻatautaia o le kainic acid.2

 

EUK-134 81065-76-1 Tusitaiala

  1. J Pharmacol Exp Ther. 1998 Ian; 284 (1): 215-21; Proc Natl Acad Sci US A. 1999 Aug 17; 96 (17): 9897-902; PLoS Tasi. 2017 Fep 2; 12 (2): e0169146; Mol Cell Biochem. 2016 Sep; 420 (1-2): 185-94.
  2. J. Ophoven et al. Salen-manganese complexes: sophisticated mea faigaluega mo le auʻiliʻiliga o intercellular ROS faʻailoga ala. Anticancer Res. 2010 Oketopa; 30 (10): 3967-79.
  3. Failli et al. O le novel manganese complex e aoga tele e pei o le superoxide anion scavenger ma le vailaʻau e faʻamalosia ai le toto mai le sela ma le tino o manuʻa manuʻa. J Med Chem. 2009 Nov 26; 52 (22): 7273-83.
  4. Decraene et al. O le synthetic superoxide dismutase / catalase mimetic (EUK-134) e taofia ai le faʻatamaia e le membrane-faʻaleagaina o auala o le protein mitini-activated protein kinase ma faʻaititia ai le faʻaputuga p53…. J Inivesi Dermatol. 2004 Fep; 122 (2): 484-91.

 

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