Stock API Raw Material Pharma Grade High Quality SR9011 CAS 1379686-29-9 Okokwakha umzimba
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Ukusetshenziswa
I-SR9011 iyi-agonist ye-REV-ERBα/β ene-IC50s ye-790 nM kanye ne-560 nM ye-REV-ERBα kanye ne-REV-ERBβ, ngokulandelanayo.Ingawelapha umdlavuza.
I-myocardial infarction ingesinye sezifo ezinezinga eliphezulu lokufa kwezifo zenhliziyo.I-infarction ye-myocardial ibangelwa ukuqina kwe-coronary artery stenosis noma i-spasm, okuholela ku-acute noma eqhubekayo ye-myocardial ischemia kanye ne-hypoxia, nokufa kweseli le-myocardial.Ama-cytokines ahlukahlukene ane-pro-inflammatory afana ne-interleukin-1β (IL-1β) kanye ne-tumor necrosis factor-α (TNF-α) ahilelekile ekulungisweni kwe-myocardial3.I-SR9011 iyi-agonist ye-REV-ERBα/β, ilungu lomndeni we-nuclear receptor, futhi izifundo zithole ukuthi ingalawula ukugaywa kwezicubu zebhayoloji.U-Huang Guodong uthole ukuthi i-SR9011 idlala indima ebalulekile ekulawuleni isigqi sezakhi zofuzo ze-autophagy ku-zebrafish.
I-C-terminus yeprotheni yomndeni ye-SR9011 ayinaso isizinda esibopha i-ligand, kodwa ingavimbela ukubonakaliswa kwephrotheni ye-Rev-erb ngokuqasha i-nuclear receptor repressor factor kanye ne-histone deacetylase 3, njll. I-Histone deacetylase 3 iyi-agonist ye-Rev-erb futhi i-molecule encane ye-chemical probe.I-Fon-taine ibike okokuqala ku-Chemicalbook ukuthi kukhona ukuhlobana phakathi kwe-SR9011 nokuvuvukala, futhi i-SR9011 ingavimbela ukuvezwa kwe-Tr4, ngaleyo ndlela ilawule isignali yokuvuvukala.Izazi zakwamanye amazwe zithole ukuthi kuma-macrophage abantu, ukukhulisa inkulumo ye-mRNA ye-SR9011 ngezindlela zemithi kuholela ngokuqondile ekwehleni kwenkulumo ye-mRNA ye-pro-inflammatory factor interleukin-6.
Okufanayo:
| 1-Pyrrolidinecarboxamide, 3-[[(4-chlorophenyl)methyl][(5-nitro-2-thienyl)methyl]amino]methyl]-N-pentyl- |
| I-SR9011 |
| I-UNII:VYI79FLZ6W |
| 3-({(4-Chlorobenzyl)[(5-nitro-2-thienyl)methyl]amino}methyl)-N-pentyl-1-pyrrolidinecarboxamide |
I-SR9011 CAS 1379686-29-9 Ucwaningo:
Ucwaningo lwe-in vitro:
I-SR9011 umthamo-oncike kumthamo okhuphukile umsebenzi wokucindezela oncike ku-REV-ERB kanye ne-RE4- Intatheli ye-luciferase ephendulayo (REV-ERBα IC50 = 790 nM, REV-ERBβ IC50 = 560 nM).I-SR9011 icindezela ngokunamandla futhi ngamandla okulotshiweyo ekuhlolweni kokudluliselwa komunye kusetshenziswa i-REV-ERBα yobude obugcwele kanye nofuzo lwentatheli ye-luciferase olushayelwa umgqugquzeli we-Bmal1 (SR9011 IC50 = 620nM).I-SR9011 ivimbela ukubonakaliswa kwe-BGAL1 mRNA kumaseli e-HepG2 ngendlela encike ku-REV-ERBα/β-[1] SR9011 ivimbela ukwanda kwemigqa yamaseli omdlavuza webele kungakhathaliseki ukuthi i-ER noma i-HER2 yabo injani.I-SR9011 ibonakala imisa kancane umjikelezo wamaseli omdlavuza webele ngaphambi kwesigaba se-M.I-Cyclin A (CCNA2) ihlonzwe njengofuzo oluqondiswe ngqo lwe-REV-ERB, okuphakamisa ukuthi ukuvinjwa kokuvezwa kwale cyclin nge-SR9011 kungase kulamule ukuboshwa komjikelezo wamaseli.Ukwelashwa nge-SR9011 kuphumele ekukhuleni kwamaseli esigabeni se-G0/G1 kanye nokuncipha kwamaseli ezigabeni ze-S ne-G2/M, okuphakamisa ukuthi ukwenziwa kusebenze kwe-REV-ERB kungase kubangele uguquko oluncishisiwe ukusuka ku-G1 ukuya ku-S isigaba kanye/noma isigaba sika-S.
Ucwaningo lomzimba:
I-SR9011 ibonise ukuchayeka kwe-plasma okunengqondo, ngakho-ke, ukubonakaliswa kwezakhi zofuzo ezisabelayo ze-REV-ERB kwahlolwa esibindini samagundane aphathwe ngemithamo ehlukene ye-SR9011 izinsuku ezingu-6.I-plasminogen activator inhibitor yohlobo 1 lofuzo (i-Serpine1) iwufuzo oluqondiwe lwe-REV-ERB futhi yabonisa ukucindezelwa kokusho okuncike kumthamo ekuphenduleni i-SR9011.I-Cholesterol 7α-hydroxylase (Cyp7a1) kanye nezakhi zofuzo ezibophezelayo ze-sterol (Srepf1) nazo zaboniswa ukuphendula ku-REV-ERB futhi zazivinjelwe ngokuncika kumthamo ngamanani akhulayo we-SR9011.Ngemuva kwezinsuku eziyi-12 ezimeni ze-D:D, amagundane ajovwa ngomthamo owodwa we-SR9011 noma imoto ku-CT6 (ukuveza okukhulu kwe-Rev-erbα).Imijovo yemoto ayizange ibangele ukuphazamiseka komsebenzi we-circadian rhythmic locomotor.Kodwa-ke, ukuphathwa komthamo owodwa we-SR9011 kubangele ukulahleka komsebenzi we-locomotor phakathi nesigaba sobumnyama sezifundo.Umsebenzi ojwayelekile ubuyela kumjikelezo we-circadian olandelayo, ohambisana nokuvunyelwa kwezidakamizwa okungaphansi kwamahora angama-24.Ngaphansi kwezimo ezimnyama eziqhubekayo, ukuncishiswa okuncike ku-SR9011 ekuziphatheni okugijima kwamasondo kumagundane kwakuncike kumthamo, futhi amandla (ED50 = 56 mg/kg) ayefana nalawo okuvinjelwa okuphakathi kwe-SR9011 kofuzo lokuphendula lwe-REV-ERB, i-Srebf1. , ku-vivo (ED50 = 67mg/kg) [1].