Alaabta

EUK-134 (81065-76-1)

EUK 134 waa ka samaysan manganese-porphyrin synthetic kaas oo loo diiwaan galiyay inuu u dhaqmo sidii qashin-qubka noocyada oksaydhiyeyaasha sida hydrogen peroxide, peroxynitrite iyo superoxide. Xaruntani waa dhisme-manganese salen ah oo wax laga beddelay si loo kordhiyo hawlaheeda catalase iyada oo la ilaalinayo dhaqdhaqaaqa SOD.

Caqligu wuxuu awood u leeyahay inuu soo saaro oo uu bixiyo tiro badan. Dhammaan wax soo saarka ee hoos yimaada xaaladda cGMP iyo nidaamka xakamaynta tayada adag, dhammaan dukumeentiyada imtixaanka iyo muunada la heli karo.
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EUK-134 budada Macluumaadka Saldhigga

magaca  EUK-134
CAS 81065-76-1
xagiisayna 98%
Magaca kiimikada chloro[[2,2′-[1,2-ethanediylbis[(nitrilo-κN)methylidyne]] bis[6-methoxyphenolato-κO]]-manganese
Isku mid ahaanshaha 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) koloride ;ETHYLBISIMINOMETHYLGUAIACOL MANGANESE KHLORIDE;chloro(bis(3,3′di-methoxysalicylidene)ethylenediamine)manganese;EUK 134, SOD/catalase mimetic, Ethylbisiminomethylguaiacol manganese chloride
Formula kelli C18H18ClMnN2O4
Miisaanka kelli 416.7
barta dhalaalaysa >300°C
Muhiimadda InChI YUZJJFWCXJDFOQ-GAMUHHASSA-K
Form Solid
Imaanshaha Budada bunni madow
Nolosha badh /
milmi Ku milmay biyaha (0.2 mg/ml at 25° C), PBS pH 7.2, ethanol, DMSO, iyo DMF.
kaydinta Xaaladda Ku kaydi -20 ° C
Codsiga EUK-134 ayaa loo isticmaalay sidii antioxidant.

EUK-134 ayaa loo isticmaalay si loo go'aamiyo habka asaasiga ah ee hypoxia-inducible factor-1a (HIF-1a) xasilinta unugyada endothelial aortic ee bini'aadamka (HAECs).

Dukumentiga Tijaabinta Available

 

EUK-134 81065-76-1 General Description

Qalab manganese salen leh oo leh superoxide dismutase (SOD) iyo sifooyinka mimetic catalase. EUK134 waxay soo bandhigtaa waxqabadyada antioxidant ee xoogga leh, waxayna joojisaa samaynta β-amyloid iyo amyloid fibril (IAPP). Qalabka dawooyinka waxtarka leh ee horumarinta xeryahooda cusub ee daaweynta Cudurka Alzheimers iyo Parkinson iyo nooca 2aad ee sonkorowga.

Unugyada SK-N-MC, EUK134 waxay ka ilaalisaa unugyada neerfayaasha ka hortagga sunta H2O2 iyadoo yaraynaysa cadaadiska oksaydhka iyada oo la joojinayo dariiqa MAPK, sidoo kale waxay keentaa hoos u dhaca muujinta pro-apoptotic genes p53 iyo Bax iyo sidoo kale muujinta kor u kaca ee anti-apoptotic Bcl- 2 hidde. Ka-hortagga EUK-134 (10 μM) waxay wax ku ool u ahayd ka hortagga isbeddellada hypertrophic ee unugyada H9C2, hoos u dhigista cadaadiska oksaydhka, iyo ka hortagga isbeddelka dheef-shiid kiimikaadka. Daawaynta EUK-134 waxay hagaajisay heerka oksaydhiyaha ee mitochondria iyo dib-u-dhigista hypertrophy-ku-dhimista awoodda xuubka mitochondrial. Ku-darka EUK-134 ayaa sidaas darteed loo aqoonsaday hab cusub oo lagu dhimayo hypertrophy wadnaha iyo amaahinta baaxadda horumarinta EUK-134 oo ah wakiilka daweynta ee maaraynta cudurrada wadnaha iyo xididdada dhiigga.

 

EUK-134 81065-76-1 Mfarsamada Of Action

Dadku waxay cunaan cunto iyo biyo maalin kasta, iyaga oo u qaada unugyo kala duwan oo jirka ah iyada oo loo marayo habka dheef-shiidka iyo habka wareegga dhiigga, oo waxay ku milmaan unugyada si ay u sii daayaan tamarta. Inta lagu jiro habka dheef-shiid kiimikaadka oo dhan, tiro badan oo ah "ROS (noocyada oksijiinta falcelinta)" ayaa la soo saari doonaa, oo ay ku jiraan: O2-, H2O2 iyo HO2-, -OH, iwm , taasoo keenta apoptosis unug iyo xitaa necrosis.

Labada qaybood ee muhiimka ah ee antioxidant ee jidhka bini'aadamka waa: superoxide dismutase (SOD) iyo catalase (CAT). Labadan qaybood ayaa si dhow u wada shaqeeya si ay u beddelaan "ROS (Reactive Oxygen Cluster)" ee lagu soo saaro habka dheef-shiid kiimikaadka biyaha iyo ogsijiinta si loo ilaaliyo dheef-shiid kiimikaadka caadiga ah ee jirka.

Miisaanka unugyadu sareeyo ee SOD awgeed, way adagtahay in la dhex galo stratum corneum. Intaa waxaa dheer, xitaa haddii SOD ay maqaarka ka soo gasho qadar yar iyada oo loo marayo daloollada iyo qanjidhada dhididka, si fudud ayaa loo nadiifiyaa borotiinka waxayna leedahay xasillooni xumo iyo dheef-shiid kiimikaad degdeg ah ee jidhka bini'aadamka. Sifooyinkan SOD waxay ka hortagayaan codsigeeda qurxinta. Sidaa darteed, "EUK-134" ayaa loo sameeyay si loogu beddelo codsiga SOD iyo CAT ee goobta qurxinta.

 

EUK-134 81065-76-1 Codsiga

Ka ilaali waxyeelada DNA-da

Dayactirka DNA

Anti-barar

anti-qayilo

Daryeelka muraayadda qorraxda, kaabi daryeelka ay maaddooyinka guud ee muraayadaha qoraxda aysan daryeeli karin

Ka-hortagga xanaaqa

La dagaallama cadaadiska oksaydhka

Ka hortagga walaaca

 

EUK-134 81065-76-1 Baadhis dheeraad ah

EUK 134 waa kakan salen-manganese oo wax laga beddelay si loo kordhiyo hawlaheeda catalase iyada oo la sii hayo dhaqdhaqaaqa SOD. EUK 134 waa dhisme-manganese salen oo wax laga beddelay si loo kordhiyo hawlaheeda catalase iyada oo la sii hayo dhaqdhaqaaqa SOD. EUK 134 waxay isticmaashaa hydrogen peroxide oo leh falcelin bilow ah oo ah 234 µM/min in vitro.1 EUK 134 waxay difaac u tahay qaabka istaroogga jiirka, iyadoo adeegsanaysa xididdada halbowlaha maskaxda ee dhexe. Marka la joogo 2.5 mg/kg, jiirka lagu daweeyay EUK 134 ayaa muujiyay hoos u dhaca mugga infarct in ka badan 80%. EUK 134 ee 10 mg/kg sidoo kale waxay si weyn u yaraynaysaa dhaawaca maskaxda ee jiirka ka dib maamulka nidaamka ee kainiga.2

 

EUK-134 81065-76-1 Tixraaca

  1. J Pharmacol Exp Ther. 1998 Jan;284(1):215-21; Proc Natl Acad Sci US A. 1999 Aug 17;96(17):9897-902; PLoS Mid. 2017 Feb 2;12(2):e0169146; Mol Cell Biochem. 2016 Seb;420 (1-2): 185-94.
  2. J. Ophoven iyo al. Guryaha Salen-manganese: Qalab casri ah oo loogu talagalay falanqaynta dariiqyada calaamadaynta intercellular ROS. Ka-hortagga kansarka Res. 2010 Oct;30 (10):3967-79.
  3. Failli iyo al. Qalab cusub oo manganese ah oo wax ku ool u ah sida superoxide anion scavenger iyo wakiilka daweynta ka hortagga unugyada iyo dhaawaca oksaydhiyaha. J Med Chem. 2009 Nof 26;52 (22):7273-83.
  4. Decraene iyo al. A synthetic superoxide dismutase / catalase mimetic (EUK-134) waxay joojisaa firfircoonida waxyeelada xuubabka ee dariiqyada kinase borotiinka firfircoon ee mitogen-ka waxayna yaraynaysaa ururinta p53…. J Maalgelinta Dermatol. 2004 Feb;122(2):484-91.

 

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