Fa'asoa API Mea Matagofie Pharma Vasega Tulaga Maualuga SR9011 CAS 1379686-29-9 Mo Fausia Tino
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Fa'aoga
SR9011 o se REV-ERBα / β agonist ma IC50s o 790 nM ma 560 nM mo REV-ERBα ma REV-ERBβ, faasologa.E mafai ona togafitia le kanesa.
Myocardial infarction o se tasi lea o faʻamaʻi e sili ona maualuga le oti o faʻamaʻi cardiovascular.O le fa'ama'i o le fatu e mafua mai i le fa'ama'i po'o le fa'ama'i o le alatoto fatu, e i'u ai i le ma'i po'o le faifai pea ole myocardial ischemia ma le hypoxia, ma le myocardial cell death.O cytokines pro-inflammatory eseese e pei ole interleukin-1β (IL-1β) ma le tumor necrosis factor-α (TNF-α) o loʻo aʻafia i le toe faʻaleleia o le myocardial3.SR9011 o se REV-ERBα / β agonist, o se sui o le aiga faaniukilia receptor, ma suʻesuʻega ua maua e mafai ona faʻatonutonuina le metabolism o mea ola.Na maua e Huang Guodong o le SR9011 e iai sona sao taua i le faʻatonutonuina o le pao o genes autophagy i zebrafish.
O le C-terminus o le protein a le aiga SR9011 e leai se ligand-binding domain, ae e mafai ona faʻalavelaveina le faʻaalia o le Rev-erb protein e ala i le suʻeina o le nuclear receptor repressor factor ma le histone deacetylase 3, ma isi. Histone deacetylase 3 o se Rev-erb agonist ma se su'esu'ega kemikolo la'ititi.Na lipotia muamua e Fon-taine i le Chemicalbook o loʻo i ai se faʻamaopoopo i le va o le SR9011 ma le mumū, ma e mafai e le SR9011 ona faʻalavelaveina le faʻaaliga o le Tr4, ma pulea ai le faʻailoga inflammatory.Ua maua e le au sikola mai fafo e faapea i macrophages tagata, faʻateleina le faʻamatalaga mRNA o le SR9011 e ala i metotia faʻafomaʻi e taʻitaʻia saʻo ai le faʻaitiitia o le faʻaaliga mRNA o le pro-inflammatory factor interleukin-6.
uiga tutusa:
| 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 Suesuega:
Su'esu'ega in vitro:
SR9011 dose-faʻalagolago faʻateleina le REV-ERB-faʻalagolago i le faʻalavelave faʻalavelave ma le RE4- Responsive luciferase reporter (REV-ERBα IC50 = 790 nM, REV-ERBβ IC50 = 560 nM).SR9011 malosi ma malosi le taofiofia o tusitusiga i se suʻesuʻega faʻatasi e faʻaaoga ai le REV-ERBα atoa faʻatasi ai ma se luciferase faʻasalalau gene faʻamalosi e le Bmal1 promoter (SR9011 IC50 = 620nM).SR9011 fa'asaina le fa'aaliga BGAL1 mRNA i sela HepG2 i se REV-ERBα/β-faalagolago [1] SR9011 fa'alavelave le fa'ateleina o laina sela o le kanesa o le susu e tusa lava po'o le a le tulaga o le ER po'o le HER2.O le SR9011 e foliga mai e taofi le taamilosaga o sela o sela o le kanesa o le susu a'o le'i o'o i le vaega M.O le Cyclin A (CCNA2) na faʻaalia o se faʻasologa saʻo o le REV-ERB, faʻapea o le taofia o le faʻaalia o lenei cyclin e le SR9011 e mafai ona faʻatalanoaina le puʻeina o le taamilosaga.Togafitiga faʻatasi ma le SR9011 na mafua ai le faʻateleina o sela i le vaega G0 / G1 ma faʻaititia sela i vaega S ma G2 / M, faʻapea o le faʻagaoioia o le REV-ERB e mafai ona faʻaitiitia ai le suiga mai le G1 i le S vaega ma / poʻo le S vaega.
Su'esu'ega fa'aletino:
O le SR9011 na faʻaalia ai le faʻaalia o le plasma talafeagai, o le mea lea, o le faʻaaliga o REV-ERB tali genes na suʻesuʻeina i ate o isumu na togafitia i tui eseese o le SR9011 mo aso 6.O le plasminogen activator inhibitor type 1 gene (Serpine1) o se REV-ERB faʻatulagaina gene ma faʻaalia le faʻaogaina o le faʻaogaina o faʻamatalaga i le tali atu i le SR9011.Cholesterol 7α-hydroxylase (Cyp7a1) ma le sterol response element binding protein (Srepf1) genes na faʻaalia foi e tali atu i le REV-ERB ma sa faʻalagolago i fua faʻatatau i le faʻateleina o le SR9011.Ina ua maeʻa aso 12 i tulaga D: D, na tui le isumu i se fua e tasi o le SR9011 poʻo le taʻavale i le CT6 (faʻaaliga maualuga o Rev-erbα).Ole tui ole ta'avale e le'i fa'alavelaveina le gaioioiga o le locomotor circadian rhythmic locomotor.Ae ui i lea, o le faʻaaogaina o se tasi fua o le SR9011 na mafua ai le leiloa o le gaioiga i le taimi o le pogisa o mataupu.O gaioiga masani e toe fo'i i le isi circadian cycle, fa'atasi ma le kilia o vaila'au e itiiti ifo i le 24 itula.I lalo o tulaga pogisa faifai pea, o le SR9011-faʻalagolago i le faʻaitiitia o le uili o le taʻavale i isumu na faʻalagolago, ma o le malosi (ED50 = 56 mg / kg) e tutusa ma le SR9011-mediated inhibition of the REV-ERB response gene, Srebf1 , in vivo (ED50 = 67mg/kg) [1].