Raw API Raw Material Pharma Grade Kounga teitei SR9011 CAS 1379686-29-9 Mo te Hanga tinana
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Whakamahinga
Ko te SR9011 he REV-ERBα / β agonist me nga IC50 o 790 nM me 560 nM mo REV-ERBα me REV-ERBβ, ia.Ka taea te rongoa mate pukupuku.
Ko te infarction myocardial tetahi o nga mate he nui rawa te mate o nga mate ngakau.Ko te paheketanga o te ngakau ka puta mai i te stenosis o te arai korokoro, i te mokowhiti ranei, ka puta mai te ischemia me te hypoxia, me te mate o te pūtau myocardial.Ko nga momo cytokine pro-inflammatory penei i te interleukin-1β (IL-1β) me te tumo necrosis factor-α (TNF-α) kei roto i te remodeling myocardial3.Ko te SR9011 he REV-ERBα/β agonist, he mema o te whanau kaiawhina karihi, a kua kitea e nga rangahau ka taea e ia te whakahaere i te whakawhitinga o nga kopa koiora.I kitea e Huang Guodong he mahi nui a SR9011 ki te whakahaere i te manawataki o nga ira autophagy i roto i te ika zebrafish.
Ko te C-terminus o te pūmua whanau SR9011 karekau he rohe herenga herenga, engari ka taea e ia te aukati i te whakapuakitanga o te pūmua Rev-erb ma te tango i te take repressor receptor karihi me te histone deacetylase 3, me etahi atu. Ko te Histone deacetylase 3 he Rev-erb agonist me he rangahau matū ngota iti.I korero tuatahi a Fon-taine i roto i te Chemicalbook he hononga kei waenganui i te SR9011 me te mumura, a ka taea e SR9011 te aukati i te whakaaturanga o Tr4, na reira ka whakahaere i te tohu mumura.Kua kitea e nga tohunga o nga iwi ke i roto i nga macrophages tangata, ko te whakanui ake i te whakaaturanga mRNA o SR9011 na roto i nga tikanga rongoa ka arahi tika ki te heke o te whakaaturanga mRNA o te take pro-inflammatory interleukin-6.
Taurite:
| 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 Rangahau:
Te rangahau in vitro:
SR9011 horopeta-ti'aturi nui ake mahi repressor whakawhirinaki REV-ERB me RE4- Responsive luciferase kairipoata (REV-ERBα IC50 = 790 nM, REV-ERBβ IC50 = 560 nM).Ko te SR9011 te kaha me te kaha ki te tarai i te tuhinga i roto i te whakamatautau whakawhiti-tahi ma te whakamahi i te REV-ERBα roa-roa me te ira kairipoata luciferase i peia e te kaiwhakatairanga Bmal1 (SR9011 IC50 = 620nM).Ka whakakorehia e te SR9011 te whakaaturanga mRNA BGAL1 i roto i nga pūtau HepG2 i roto i te REV-ERBα/β-ti'aturi [1] SR9011 te aukati i te tipu o nga raina pukupuku pukupuku pukupuku ahakoa te ahua o te ER, HER2 ranei.Ko te ahua o te SR9011 ka whakataa i te huringa pūtau o nga pūtau mate pukupuku uma i mua i te wahanga M.Ko te Cyclin A (CCNA2) i tohuhia he ira whainga tika o REV-ERB, e kii ana ko te aukati i te whakaputanga o tenei paihikara e SR9011 ka taea te takawaenga i te hopu huringa pūtau.Ko te maimoatanga me te SR9011 ka piki ake nga pūtau i roto i te wahanga G0 / G1 me te heke o nga pūtau i roto i nga wahanga S me G2 / M, e kii ana ko te whakahohenga o te REV-ERB ka puta he iti ake te whakawhiti mai i te G1 ki te wahanga S me te waahanga S ranei.
Rangahau tinana:
I whakaatu a SR9011 i te whakaaturanga plasma whaitake, na reira, i tirotirohia te whakaaturanga o nga ira urupare REV-ERB i roto i nga ate o nga kiore i tukinotia ki nga momo rereke o SR9011 mo nga ra 6.Ko te ira momo 1 te ira whakakaha plasminogen (Serpine1) he ira whainga REV-ERB me te whakaatu i te aukati inenga-whakaaro o te korero hei whakautu ki te SR9011.Ko te Cholesterol 7α-hydroxylase (Cyp7a1) me te sterol whakautu huānga here pūmua (Srepf1) i whakaatuhia hoki ki te urupare ki te REV-ERB me te aukati i te horopeta me te piki haere o te SR9011.I muri i nga ra 12 i roto i nga tikanga D: D, ka werohia nga kiore ki te horopeta kotahi o te SR9011, te waka ranei i te CT6 (te korero teitei o Rev-erbα).Karekau nga werohanga waka i whakararu i te mahi o te circadian rhythmic locomotor.Heoi, ko te whakahaerenga o te horopeta kotahi o te SR9011 i mate ai te mahi a-roto i te waa pouri o nga kaupapa.Ka hoki mai te ngohe noa ki te huringa circadian e whai ake nei, e rite ana ki te whakakorenga raau taero iti iho i te 24 haora.I raro i nga ahuatanga pouri tonu, ko te whakahekenga o te SR9011 i roto i te whakahaere wira i roto i nga kiore i whakawhirinaki ki te horopeta, a ko te kaha (ED50 = 56 mg / kg) he rite ki te SR9011-whakawhitiwhiti i te ira whakautu REV-ERB, Srebf1 , in vivo (ED50 = 67mg/kg) [1].