Ububiko API Raw Ibikoresho Farma Icyiciro Cyiza SR9011 CAS 1379686-29-9 Kubaka umubiri
Menyesha:
Email:ceo66@hbainuodi.com
Whatsapp / Skape: +8618849057872
Wickr: alice868
Ikoreshwa
SR9011 ni REV-ERBα / β agonist hamwe na IC50s ya 790 nM na 560 nM kuri REV-ERBα na REV-ERBβ.Irashobora kuvura kanseri.
Indwara ya Myocardial ni imwe mu ndwara zifite umubare munini w'impfu z'indwara z'umutima.Indwara ya Myocardial iterwa na coronary arteri stenosis cyangwa spasm, bikaviramo ischemia myocardial ischemia na hypoxia ikaze cyangwa ikomeza, hamwe na selile myocardial.Cytokine zitandukanye zitera inflammatory nka interleukin-1β (IL-1β) hamwe na tumorosi nekrosis-α (TNF-α) igira uruhare mu kuvugurura myocardial3.SR9011 ni REV-ERBα / β agonist, umwe mu bagize umuryango wakira ibyuka bya kirimbuzi, kandi ubushakashatsi bwerekanye ko bushobora kugenga metabolisme y’imitsi y’ibinyabuzima.Huang Guodong yasanze SR9011 igira uruhare runini mugutunganya injyana ya gen autophagy muri zebrafish.
C. umuto muto wa molekile.Fon-taine yabanje gutangaza muri Chemical Book ko hari isano hagati ya SR9011 n’umuriro, kandi SR9011 irashobora kubuza imvugo ya Tr4, bityo ikagenzura ibimenyetso byaka umuriro.Intiti z’amahanga zasanze muri macrophage zabantu, kongera imvugo ya mRNA ya SR9011 hakoreshejwe uburyo bwa farumasi biganisha ku kugabanuka kwimvugo ya mRNA yerekana ibintu bitera interleukin-6.
Synonyme ：
| 1-Pyrrolidinecarboxamide, 3 - [[[((4-chlorophenyl) methyl]] |
| SR9011 |
| UNII: VYI79FLZ6W |
| 3 - ({(4-Chlorobenzyl) [(5-nitro-2-thienyl) methyl] amino} methyl) -N-pentyl-1-pyrrolidinecarboxamide |
SR9011 CAS 1379686-29-9 Ubushakashatsi:
Mu bushakashatsi bwa vitro ：
SR9011 ikigereranyo cyiyongereye kubikorwa bya repressor ya REV-ERB na RE4- Umunyamakuru wa luciferase yitabira (REV-ERBα IC50 = 790 nM, REV-ERBβ IC50 = 560 nM).SR9011 ikomeye kandi ikomeye ihagarika inyandiko mvugo muguhuza hamwe hakoreshejwe uburebure bwuzuye REV-ERBα hamwe numunyamakuru wa luciferase gene utwarwa na Bmal1 promoter (SR9011 IC50 = 620nM).SR9011 ibuza imvugo ya BGAL1 mRNA mu ngirabuzimafatizo za HepG2 mu buryo buterwa na REV-ERBα / β [1] SR9011 ibuza ikwirakwizwa ry'imirongo ya kanseri y'ibere utitaye ku miterere ya ER cyangwa HER2.SR9011 isa nkaho ihagarika ingirabuzimafatizo ya kanseri y'ibere mbere yicyiciro cya M.Cyclin A (CCNA2) yamenyekanye nka gen igamije intego ya REV-ERB, byerekana ko kubuza iyi cyclin na SR9011 bishobora guhuza ifatwa ry’akagari.Umuti hamwe na SR9011 watumye selile ziyongera mugice cya G0 / G1 no kugabanuka kwingirabuzimafatizo mugice cya S na G2 / M, byerekana ko gukora REV-ERB bishobora gutuma kugabanuka kuva kuri G1 kugera kuri S na / cyangwa S.
Ubushakashatsi ku mubiri ：
SR9011 yerekanye plasma igaragara neza, kubwibyo, imvugo ya gen yitabira ya REV-ERB yasuzumwe mu mbeba yimbeba zavuwe na dosiye zitandukanye za SR9011 muminsi 6.Imikorere ya plasminogen inhibitor yo mu bwoko bwa 1 (Serpine1) ni gene ya REV-ERB kandi yerekanaga gukandamizwa gukabije kwamagambo asubiza SR9011.Cholesterol 7α-hydroxylase (Cyp7a1) hamwe na sterol yo gusubiza ingirabuzimafatizo ya poroteyine (Srepf1) nazo zerekanwe ko zisubiza REV-ERB kandi zarahagaritswe cyane bitewe na SR9011.Nyuma yiminsi 12 mubihe D: D, imbeba zatewe inshinge imwe ya SR9011 cyangwa imodoka kuri CT6 (imvugo yo hejuru ya Rev-erbα).Gutera ibinyabiziga ntabwo byaviriyemo guhagarika ibikorwa bya circadian rhythmic lokomoteri.Nyamara, imiyoborere yikinini kimwe cya SR9011 yatumye habaho gutakaza ibikorwa bya lokomoteri mugihe cyumwijima.Ibikorwa bisanzwe bigaruka kumuzingo ukurikiraho, bigendana no gukuraho ibiyobyabwenge bitarenze amasaha 24.Mugihe cyumwijima uhoraho, kugabanuka kwa SR9011 kugabanuka kwimyitwarire yimodoka mu mbeba byari biterwa na dose, kandi imbaraga (ED50 = 56 mg / kg) zasaga nubwa SR9011-yabujijwe kubuza gene igisubizo cya REV-ERB, Srebf1 , muri vivo (ED50 = 67mg / kg) [1].