Stock API Raw Material Pharma Grade High Quality SR9011 CAS 1379686-29-9 Yomanga thupi
Ndiuzeni:
Email:ceo66@hbainuodi.com
Whatsapp/Skape:+8618849057872
Wickr: alice868
Kugwiritsa ntchito
SR9011 ndi REV-ERBα/β agonist yokhala ndi IC50s ya 790 nM ndi 560 nM ya REV-ERBα ndi REV-ERBβ, motsatana.Amatha kuchiza khansa.
Myocardial infarction ndi amodzi mwa matenda omwe amafa kwambiri chifukwa cha matenda amtima.Myocardial infarction imayamba chifukwa cha kutsika kwa mitsempha yam'mitsempha yamagazi kapena kupindika, zomwe zimapangitsa kuti pachimake kapena kupitilirabe myocardial ischemia ndi hypoxia, komanso kufa kwa maselo a myocardial.Ma cytokines osiyanasiyana oletsa kutupa monga interleukin-1β (IL-1β) ndi tumor necrosis factor-α (TNF-α) amakhudzidwa ndi kukonzanso kwa myocardial3.SR9011 ndi REV-ERBα / β agonist, membala wa banja la nyukiliya receptor, ndipo kafukufuku wapeza kuti akhoza kulamulira kagayidwe kake ka tizilombo toyambitsa matenda.Huang Guodong adapeza kuti SR9011 imagwira ntchito yofunika kwambiri pakuwongolera kayimbidwe ka majini a autophagy mu zebrafish.
C-terminus ya SR9011 puloteni ya banja ilibe malo omangira ligand, koma imatha kulepheretsa kufotokoza kwa mapuloteni a Rev-erb polemba nyukiliya receptor repressor factor ndi histone deacetylase 3, etc. Histone deacetylase 3 ndi Rev-erb agonist ndi kachipangizo kakang'ono ka molekyulu.Fon-taine adanenedwa koyamba mu Chemicalbook kuti pali kulumikizana pakati pa SR9011 ndi kutupa, ndipo SR9011 imatha kuletsa mawu a Tr4, potero kuwongolera chizindikiro chotupa.Akatswiri akunja apeza kuti mu ma macrophages aumunthu, kukulitsa mawu a mRNA a SR9011 mwa njira zamankhwala kumabweretsa kutsika kwa mRNA kufotokoza kwa pro-inflammatory factor interleukin-6.
Mawu ofanana:
| 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 Kafukufuku:
Kafukufuku wa in vitro:
SR9011 mlingo-wodalira kuchuluka kwa REV-ERB-odalira repressor ntchito ndi RE4- Responsive luciferase reporter (REV-ERBα IC50 = 790 nM, REV-ERBβ IC50 = 560 nM).SR9011 molimba mtima komanso molimba mtima imapondereza zolembedwa poyeserera kophatikizana pogwiritsa ntchito REV-ERBα yayitali komanso jini ya mtolankhani wa luciferase yoyendetsedwa ndi wolimbikitsa Bmal1 (SR9011 IC50 = 620nM).SR9011 imalepheretsa BGAL1 mRNA kufotokoza m'maselo a HepG2 mu REV-ERBα / β-odalira njira [1] SR9011 imalepheretsa kufalikira kwa maselo a khansa ya m'mawere mosasamala kanthu za ER kapena HER2.SR9011 ikuwoneka kuti imayimitsa kuzungulira kwa ma cell a khansa ya m'mawere gawo la M lisanachitike.Cyclin A (CCNA2) idadziwika ngati jini yolunjika mwachindunji ya REV-ERB, kutanthauza kuti kuletsa kufotokoza kwa cyclin ndi SR9011 kungathe kuyimira kumangidwa kwa cell.Kuchiza ndi SR9011 kunapangitsa kuti maselo achuluke mu gawo la G0/G1 ndi kuchepa kwa maselo mu magawo a S ndi G2/M, kutanthauza kuti kutsegula kwa REV-ERB kungapangitse kusintha kochepa kuchokera ku G1 kupita ku S ndi / kapena S gawo.
Kafukufuku wakuthupi:
SR9011 inawonetsa kuwonetseredwa koyenera kwa plasma, motero, mafotokozedwe a majini omvera a REV-ERB adawunikidwa m'chiwindi cha mbewa zomwe zimathandizidwa ndi mitundu yosiyanasiyana ya SR9011 kwa masiku 6.The plasminogen activator inhibitor type 1 gene (Serpine1) ndi REV-ERB chandamale jini ndipo anasonyeza kudalira mlingo kupondereza mawu poyankha SR9011.Cholesterol 7α-hydroxylase (Cyp7a1) ndi sterol reaction element yomanga mapuloteni (Srepf1) majini adawonetsedwanso kuti ayankhe REV-ERB ndipo anali oletsedwa modalira mlingo ndi kuchuluka kwa SR9011.Pambuyo pa masiku a 12 mu D: D mikhalidwe, mbewa zinabayidwa ndi mlingo umodzi wa SR9011 kapena galimoto pa CT6 (mawonekedwe apamwamba a Rev-erbα).Majekeseni agalimoto sanabweretse kusokoneza kwa circadian rhythmic locomotor ntchito.Komabe, kugwiritsa ntchito mlingo umodzi wa SR9011 kunapangitsa kuti ntchito za locomotor ziwonongeke panthawi yamdima ya ophunzirawo.Zochitika zachizolowezi zimabwereranso ku circadian cycle yotsatira, yogwirizana ndi chilolezo cha mankhwala osakwana maola 24.Pansi pamikhalidwe yamdima nthawi zonse, kutsika kodalira kwa SR9011 pamachitidwe oyendetsa magudumu mu mbewa kunali kodalira mlingo, ndipo potency (ED50 = 56 mg / kg) inali yofanana ndi ya SR9011-mediated inhibition ya REV-ERB response gene, Srebf1. , mu vivo (ED50 = 67mg/kg) [1].