Kaydka API Qalabka Farmashiyaha ceeriin Heerka Tayada Sare SR9011 CAS 1379686-29-9 ee Dhismaha Jirka
ila soo xidhiidh:
Email:ceo66@hbainuodi.com
Whatsapp/Skape:+8618849057872
Wickr:alice868
Isticmaalka
SR9011 waa REV-ERBα/β agonist leh IC50s ee 790 nM iyo 560 nM ee REV-ERBα iyo REV-ERBβ, siday u kala horreeyaan.Wuxuu daweyn karaa kansarka.
Wadnaha wadnaha waa mid ka mid ah cudurrada heerka dhimashada ugu badan ee cudurada wadnaha.Wadnaha wadnaha waxaa sababa halbowleyaasha halbowlaha wadnaha ama spasm, taasoo keenta ischemia ba'an ama joogto ah iyo hypoxia, iyo dhimashada unugyada myocardial.Cytokines pro-bararka kala duwan sida interleukin-1β (IL-1β) iyo buro necrosis factor-α (TNF-α) ayaa ku lug leh dib-u-habaynta myocardial3.SR9011 waa REV-ERBα/β agonist, xubin ka tirsan qoyska reseptor nukliyeerka, iyo daraasado ayaa lagu ogaaday in ay nidaamin karto dheef-shiid kiimikaadka unugyada noolaha.Huang Guodong wuxuu ogaaday in SR9011 ay door muhiim ah ka ciyaarto nidaaminta laxanka hiddo-wadaha autophagy ee zebrafish.
C-terminus ee borotiinka qoyska SR9011 ayaa ka maqan domain-ku-xidhan, laakiin waxay joojin kartaa muujinta borotiinka Rev-erb iyadoo la qorayo factor repressor respector nuclear iyo histone deacetylase 3, iwm. Histone deacetylase 3 waa agonist Rev-erb iyo baaritaan kiimikaad molecule yar.Fon-taine ayaa markii ugu horreysay ku sheegtay Buuga Kiimikada in uu jiro xiriir ka dhexeeya SR9011 iyo caabuqa, iyo SR9011 waxay joojin kartaa muujinta Tr4, iyada oo la xakameynayo calaamadaha caabuqa.Culimada ajnabiga ah waxay ogaadeen in macrophages bini'aadamka, kordhinta muujinta mRNA ee SR9011 ee hababka dawooyinka ayaa si toos ah u horseedaya hoos u dhaca muujinta mRNA ee factor pro-inflammatory interleukin-6.
La mid ah:
| 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 Cilmi-baaris:
Cilmi-baarista faytroogga:
Qiyaasta SR9011-ku-tiirsanaanta ayaa kordhay REV-ERB-ku-tiirsanaanta dhaqdhaqaaqa cadaadiska iyo RE4-Responsive luciferase reporter (REV-ERBα IC50 = 790 nM, REV-ERBβ IC50 = 560 nM).SR9011 waxay si xoog leh oo xoog leh u xakameysaa qorista baaritaanka isdhaafsiga iyadoo la adeegsanayo REV-ERBα dherer buuxa oo ay weheliso hidda-wadaha wariyaha luciferase ee uu wado horumariyaha Bmal1 (SR9011 IC50 = 620nM).SR9011 waxay joojisaa muujinta BGAL1 mRNA ee unugyada HepG2 qaab REV-ERBα / β-ku-tiirsanaanta [1] SR9011 waxay joojisaa fidinta khadadka unugyada kansarka naasaha iyada oo aan loo eegin xaaladooda ER ama HER2.SR9011 waxay u muuqataa inay hakisay wareegga unugyada unugyada kansarka naasaha ka hor marxaladda M.Cyclin A (CCNA2) waxaa loo aqoonsaday hidde-sidaha tooska ah ee REV-ERB, isagoo soo jeedinaya in xannibaadda muujinta wareeggan ee SR9011 ay dhexdhexaadin karto xiritaanka wareegga unugyada.Daaweynta SR9011 waxay keentay unugyo kordhay oo ku jira marxaladda G0 / G1 iyo hoos u dhaca unugyada S iyo G2 / M, taas oo soo jeedinaysa in firfircoonida REV-ERB ay keeni karto hoos u dhac ku yimaada marxaladda G1 ilaa S iyo / ama S.
Cilmi-baadhis jidheed:
SR9011 waxay muujisay soo-gaadhis plasma macquul ah, sidaa darteed, muujinta hiddo-wadaha jawaabta REV-ERB ayaa lagu baadhay beerka jiirarka oo lagu daweeyay qiyaaso kala duwan oo SR9011 ah 6 maalmood.Xakameeyaha plasminogen activator nooca 1 hidda-wadaha (Serpine1) waa hidda-wadaha bartilmaameedka REV-ERB wuxuuna muujiyay cadaadiska qiyaasta ku-tiirsanaanta muujinta jawaabta SR9011.Kolestaroolka 7a-hydroxylase (Cyp7a1) iyo unugyada jawaab-celinta sterol-ka ee borotiinka (Srepf1) ayaa sidoo kale la muujiyay inay ka jawaabaan REV-ERB waxaana si ku-tiirsan loo xaddiday iyadoo la kordhinayo qaddarka SR9011.Ka dib 12 maalmood ee xaaladaha D: D, jiirarka ayaa lagu duray hal qiyaas SR9011 ama baabuur CT6 (muujinta ugu sarreysa ee Rev-erbα).Cirbadaha baabuurka ma keenin carqaladaynta dhaqdhaqaaqa laxanka wareegga wareegga.Si kastaba ha ahaatee, maamulka hal qiyaas oo SR9011 ah ayaa keentay luminta dhaqdhaqaaqa lugaha inta lagu jiro marxaladda mugdiga ah ee mawduucyada.Dhaqdhaqaaqa caadiga ah wuxuu ku soo noqdaa wareegga wareegga xiga, oo waafaqsan nadiifinta daroogada wax ka yar 24 saacadood.Xaaladaha mugdiga ah ee joogtada ah, SR9011-ku-tiirsanaanta ku-tiirsanaanta dabeecadda orodka taayirrada ee jiirarka waxay ahayd qiyaas-ku-tiirsane, iyo awoodda (ED50 = 56 mg/kg) waxay la mid tahay tan SR9011-dhexdhexaadin ee xannibaadda jawaabta REV-ERB, Srebf1 , gudaha vivo (ED50 = 67mg/kg) [1].