Stock API Raw Material Pharma Grade High Quality SR9011 CAS 1379686-29-9 Bakeng sa Kaho ea 'Mele
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Tšebeliso
SR9011 ke REV-ERBα/β agonist e nang le IC50s ea 790 nM le 560 nM bakeng sa REV-ERBα le REV-ERBβ, ka ho latellana.E ka phekola mofetše.
Myocardial infarction ke e 'ngoe ea mafu a nang le sekhahla se phahameng sa lefu la mafu a pelo le methapo.Myocardial infarction e bakoa ke "coronary artery stenosis" kapa spasm, e bakang ho hlobaetsang kapa ho phehellang ha myocardial ischemia le hypoxia, le lefu la lisele tsa myocardial.Li-cytokine tse sa tšoaneng tsa pro-inflammatory tse kang interleukin-1β (IL-1β) le tumor necrosis factor-α (TNF-α) li ameha ho lokisoeng ha myocardial3.SR9011 ke REV-ERBα/β agonist, setho sa lelapa la nuclear receptor, 'me liphuputso li fumane hore e ka laola metabolism ea likokoana-hloko tsa likokoana-hloko.Huang Guodong o fumane hore SR9011 e bapala karolo ea bohlokoa ho laola morethetho oa liphatsa tsa lefutso tsa autophagy ho zebrafish.
C-terminus ea protheine ea lelapa ea SR9011 ha e na sebaka se tlamang ligand, empa e ka thibela polelo ea protheine ea Rev-erb ka ho hira nuclear receptor repressor factor le histone deacetylase 3, joalo-joalo Histone deacetylase 3 ke Rev-erb agonist le molek'hule e nyenyane ea ho hlahloba lik'hemik'hale.Fon-taine e tlalehile ka lekhetlo la pele ho Chemicalbook hore ho na le kamano pakeng tsa SR9011 le ho ruruha, 'me SR9011 e ka thibela polelo ea Tr4, kahoo e laola letšoao la ho ruruha.Litsebi tsa linaha tse ling li fumane hore ho macrophages ea batho, ho eketsa polelo ea mRNA ea SR9011 ka mekhoa ea phekolo ea meriana ka ho toba ho lebisa ho fokotseha ha polelo ea mRNA ea pro-inflammatory factor interleukin-6.
Synonymous:
| 1-Pyrrolidinecarboxamide, 3-[[(4-chlorophenyl)methyl][(5-nitro-2-thienyl)methyl]amino]methyl]-N-pentyl- |
| SR9011 |
| UNII: VYI79FLZ6W |
| 3-({(4-Chlorobenzyl)[(5-nitro-2-thienyl)methyl]amino}methyl)-N-pentyl-1-pyrrolidinecarboxamide |
SR9011 CAS 1379686-29-9 Lipatlisiso:
Lipatlisiso tsa in vitro:
SR9011 e itšetlehileng ka tekanyo ea tekanyo e eketsehile ts'ebetso ea khatello e itšetlehileng ka REV-ERB le RE4- moqolotsi oa litaba oa luciferase ea arabelang (REV-ERBα IC50 = 790 nM, REV-ERBβ IC50 = 560 nM).SR9011 e hatella mongolo ka mokhoa o matla le ka matla tekong ea phetisetso e sebelisa REV-ERBα ea bolelele bo felletseng hammoho le mofuta oa moqolotsi oa luciferase o tsamaisoang ke mothetsi oa Bmal1 (SR9011 IC50 = 620nM).SR9011 e thibela polelo ea BGAL1 mRNA liseleng tsa HepG2 ka mokhoa o itšetlehileng ka REV-ERBα / β [1] SR9011 e thibela ho ata ha lisele tsa kankere ea matsoele ho sa tsotellehe boemo ba bona ba ER kapa HER2.SR9011 e bonahala e emisa potoloho ea lisele tsa mofetše oa matsoele pele ho karolo ea M.Cyclin A (CCNA2) e khethiloe e le mofuta o tobileng oa REV-ERB, e fana ka maikutlo a hore ho thibela polelo ea cyclin ena ka SR9011 ho ka 'na ha e-ba lipakeng tsa ho tšoaroa ha lisele.Kalafo e nang le SR9011 e entse hore lisele li eketsehe karolong ea G0/G1 le lisele tse fokotsehileng likarolong tsa S le G2/M, ho fana ka maikutlo a hore ts'ebetso ea REV-ERB e ka fella ka phetoho e fokotsehileng ho tloha G1 ho ea ho S le / kapa S phase.
Patlisiso ea 'mele:
SR9011 e bontšitse tlhahiso e utloahalang ea plasma, ka hona, polelo ea liphatsa tsa lefutso tse arabelang tsa REV-ERB e ile ea hlahlojoa sebeteng sa litoeba tse tšoaroang ka tekanyo e fapaneng ea SR9011 bakeng sa matsatsi a 6.Mofuta oa 1 oa mofuta oa plasminogen activator inhibitor (Serpine1) ke mofuta oa sepheo sa REV-ERB 'me o bontšitse khatello ea maikutlo e itšetlehileng ka tekanyo ho arabela SR9011.Cholesterol 7α-hydroxylase (Cyp7a1) le liphatsa tsa lefutso tsa sterol tse tlamang protheine (Srepf1) li ile tsa boela tsa bontšoa hore li arabela ho REV-ERB 'me li ne li thibetsoe ho itšetlehile ka tekanyo ea tekanyo e ntseng e eketseha ea SR9011.Ka mor'a matsatsi a 12 maemong a D: D, litoeba li ne li kenngoa ka tekanyo e le 'ngoe ea SR9011 kapa koloi ho CT6 (peak expression of Rev-erbα).Liente tsa koloi ha lia ka tsa fella ka tšitiso ea tšebetso ea circadian rhythmic locomotor.Leha ho le joalo, tsamaiso ea tekanyo e le 'ngoe ea SR9011 e bakile tahlehelo ea ts'ebetso ea locomotor nakong ea lefifi la barupeluoa.Ts'ebetso e tloaelehileng e khutlela potolohong e latelang ea circadian, e tsamaellanang le ho tlosoa ha lithethefatsi nako e ka tlase ho lihora tse 24.Tlas'a maemo a lefifi a sa khaotseng, phokotso e itšetlehileng ka SR9011 ea boitšoaro ba mabili ho litoeba e ne e itšetlehile ka tekanyo ea tekanyo, 'me potency (ED50 = 56 mg / kg) e ne e tšoana le ea SR9011-mediated inhibition ea REV-ERB gene ea karabo, Srebf1. , ka vivo (ED50 = 67mg/kg) [1].