Stock API Raw Material I-Pharma iBanga loMgangatho oPhezulu SR9011 CAS 1379686-29-9 yoKwakha umzimba
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Ukusetyenziswa
I-SR9011 yi-REV-ERBα / β agonist ene-IC50s ye-790 nM kunye ne-560 nM ye-REV-ERBα kunye ne-REV-ERBβ, ngokulandelanayo.Unokuwunyanga umhlaza.
I-Myocardial infarction sesinye sezifo ezinezinga eliphezulu lokufa kwezifo zentliziyo.I-Myocardial infarction ibangelwa yi-coronary artery stenosis okanye i-spasm, ekhokelela kwi-acute okanye eqhubekayo ye-myocardial ischemia kunye ne-hypoxia, kunye nokufa kweeseli ze-myocardial.I-cytokines ehlukeneyo ye-pro-inflammatory efana ne-interleukin-1β (IL-1β) kunye ne-tumor necrosis factor-α (TNF-α) ibandakanyeka kwi-myocardial remodeling3.I-SR9011 yi-REV-ERBα/β agonist, ilungu lentsapho ye-nuclear receptor, kwaye izifundo zifumene ukuba ziyakwazi ukulawula i-metabolism yezicubu ze-biological.U-Huang Guodong ufumene ukuba i-SR9011 idlala indima ebalulekileyo ekulawuleni isingqisho se-autophagy genes kwi-zebrafish.
I-C-terminus yeprotheni yentsapho ye-SR9011 ayinayo i-domain-binding domain, kodwa inokuthintela ukubonakaliswa kweprotheni ye-Rev-erb ngokugaya i-nuclear receptor repressor factor kunye ne-histone deacetylase 3, njl njl. I-Histone deacetylase 3 i-Rev-erb agonist kunye imolekyuli encinci probe yemichiza.I-Fon-taine ixelwe okokuqala kwi-Chemicalbook ukuba kukho ulungelelwaniso phakathi kwe-SR9011 kunye nokuvuvukala, kwaye i-SR9011 inokuthintela ukubonakaliswa kwe-Tr4, ngaloo ndlela ilawula umqondiso wokuvuvukala.Abaphengululi bamazwe angaphandle baye bafumanisa ukuba kwii-macrophages zabantu, ukwandisa i-mRNA ibonakaliso ye-SR9011 ngeendlela ze-pharmacological ngokuthe ngqo kukhokelela ekunciphiseni ukubonakaliswa kwe-mRNA ye-pro-inflammatory factor interleukin-6.
Isithethantonye:
| I-1-Pyrrolidinecarboxamide, 3-[[(4-chlorophenyl)methyl][(5-nitro-2-thienyl)methyl]amino]methyl]-N-pentyl- |
| SR9011 |
| I-UNII:VYI79FLZ6W |
| 3-({(4-Chlorobenzyl)[(5-nitro-2-thienyl)methyl]amino}methyl)-N-pentyl-1-pyrrolidinecarboxamide |
SR9011 CAS 1379686-29-9 Uphando:
Uphando lwe-in vitro:
I-SR9011 i-dose-ixhomekeke kwi-dose exhomekeke kwi-REV-ERB-exhomekeke kumsebenzi wokunciphisa kunye ne-RE4- Intatheli ye-luciferase ephendulayo (REV-ERBα IC50 = 790 nM, REV-ERBβ IC50 = 560 nM).I-SR9011 icinezela ngokufanelekileyo nangokunamandla ukukhutshelwa kwi-co-transfection assay usebenzisa ubude obugcweleyo be-REV-ERBα kunye ne-luciferase reporter gene eqhutywa ngumgqugquzeli we-Bmal1 (SR9011 IC50 = 620nM).I-SR9011 inqanda ukubonakaliswa kwe-BGAL1 mRNA kwiiseli ze-HepG2 ngendlela ye-REV-ERBα / β-exhomekeke [1] SR9011 inqanda ukwanda kwemigca yeseli yomhlaza webele kungakhathaliseki ukuba i-ER okanye i-HER2 yabo.I-SR9011 ibonakala inqumama umjikelo weseli yeeseli zomhlaza wamabele phambi kwesigaba se-M.I-Cyclin A (CCNA2) ichongiwe njengejeni ekujoliswe kuyo ngokuthe ngqo ye-REV-ERB, ecebisa ukuba ukuvinjelwa kokubonakaliswa kwale cyclin nge-SR9011 kunokungenelela ukubanjwa komjikelo weseli.Unyango kunye ne-SR9011 kubangele ukwanda kweeseli kwisigaba se-G0 / G1 kunye nokunciphisa iiseli kwizigaba ze-S kunye ne-G2 / M, ezibonisa ukuba ukusebenza kwe-REV-ERB kunokubangela utshintsho oluncitshisiweyo ukusuka kwi-G1 ukuya kwi-S isigaba kunye / okanye isigaba se-S.
Uphando lomzimba:
I-SR9011 ibonise ukubonakaliswa kwe-plasma okufanelekileyo, ngoko ke, ukubonakaliswa kwe-REV-ERB yofuzo ephendulayo kwavavanywa kwisibindi seegundane eziphathwe ngamayeza ahlukeneyo e-SR9011 kwiintsuku ze-6.I-plasminogen activator inhibitor uhlobo lwe-1 gene (i-Serpine1) yi-REV-ERB ye-target gene kwaye ibonise ukunyanzeliswa kwe-dose exhomekeke kwi-dose ekuphenduleni i-SR9011.I-Cholesterol 7α-hydroxylase (Cyp7a1) kunye ne-sterol response element i-protein ebopha i-protein (i-Srepf1) izakhi zofuzo nazo zaboniswa ukuphendula kwi-REV-ERB kwaye zixhomekeke kwi-dose-inhibited kunye nezixa ezikhulayo ze-SR9011.Emva kweentsuku ze-12 kwiimeko ze-D: D, iigundane zafakwa nge-dose enye ye-SR9011 okanye isithuthi kwi-CT6 (inkcazo ephezulu ye-Rev-erbα).Iinaliti zemoto azizange zibangele ukuphazamiseka komsebenzi we-circadian rhythmic locomotor.Nangona kunjalo, ukulawulwa kwedosi enye ye-SR9011 kukhokelele kwilahleko yomsebenzi welocomotor ngexesha lesigaba sobumnyama sezifundo.Umsebenzi oqhelekileyo ubuyela kumjikelo olandelayo we-circadian, ohambelana nokukhutshwa kweziyobisi ngaphantsi kweeyure ze-24.Ngaphantsi kweemeko ezihlala zimnyama, ukucutha okuxhomekeke kwi-SR9011 ekuqhutyweni kwevili kwiigundane kwakuxhomekeke kwi-dose, kwaye amandla (ED50 = 56 mg / kg) ayefana ne-SR9011-mediated inhibition ye-REV-ERB gene yokuphendula, i-Srebf1. , kwi-vivo (ED50 = 67mg / kg) [1].