Hannun jari API Raw Material Pharma Grade High Quality SR9011 CAS 1379686-29-9 Don Gina Jiki
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Amfani
SR9011 shine REV-ERBα/β agonist tare da IC50s na 790 nM da 560 nM don REV-ERBα da REV-ERBβ, bi da bi.Zai iya magance ciwon daji.
Ciwon zuciya na daya daga cikin cututtukan da ke da yawan mace-mace na cututtukan zuciya.Rashin ciwon zuciya yana faruwa ne ta hanyar bugun jini na jijiyoyin jini ko spasm, wanda ke haifar da myocardial ischemia da hypoxia mai tsanani ko mai tsanani, da mutuwar kwayar cutar ta myocardial.Daban-daban cytokines pro-mai kumburi irin su interleukin-1β (IL-1β) da ƙari necrosis factor-α (TNF-α) suna da hannu a cikin sake fasalin myocardial3.SR9011 shine REV-ERBα / β agonist, memba ne na dangin mai karɓar nukiliya, kuma binciken ya gano cewa yana iya daidaita metabolism na kyallen takarda.Huang Guodong ya gano cewa SR9011 yana taka muhimmiyar rawa wajen daidaita tsarin kwayoyin halittar autophagy a cikin zebrafish.
C-terminus na furotin iyali na SR9011 ba shi da wani yanki mai ɗaure ligand, amma yana iya hana bayyanar furotin Rev-erb ta hanyar daukar nauyin mai karɓar mai karɓa na nukiliya da histone deacetylase 3, da dai sauransu Histone deacetylase 3 shine Rev-erb agonist kuma karamin binciken sinadarai na kwayoyin halitta.Fon-taine ya fara ba da rahoto a cikin littafin Chemical cewa akwai alaƙa tsakanin SR9011 da kumburi, kuma SR9011 na iya hana furcin Tr4, ta haka yana sarrafa siginar kumburi.Masanan kasashen waje sun gano cewa a cikin macrophages na ɗan adam, haɓaka maganganun mRNA na SR9011 ta hanyoyin magunguna kai tsaye yana haifar da raguwa a cikin maganganun mRNA na pro-inflammatory factor interleukin-6.
m:
| 1-Pyrrolidinecarboxamide, 3-[[[(4-chlorophenyl) methyl] [(5-nitro-2-thienyl) methyl] amino] methyl] -N-pentyl- |
| Saukewa: SR9011 |
| Saukewa: VYI79FLZ6W |
| 3- ({(4-Chlorobenzyl) [(5-nitro-2-thienyl) methyl] amino}methyl-N-pentyl-1-pyrrolidinecarboxamide |
SR9011 CAS 1379686-29-9 Bincike:
Binciken In vitro:
SR9011 kashi-dogara ya karu REV-ERB-dogara repressor aiki da RE4-Responsive luciferase reporter (REV-ERBα IC50 = 790 nM, REV-ERBβ IC50 = 560 nM).SR9011 da ƙarfi kuma da ƙarfi yana jujjuya rubutu a cikin gwajin haɗin gwiwa ta amfani da cikakken tsawon REV-ERBα tare da jigilar mai ba da rahoto na luciferase wanda mai haɓaka Bmal1 (SR9011 IC50 = 620nM).SR9011 yana hana BGAL1 mRNA magana a cikin sel HepG2 a cikin hanyar REV-ERBα / β-dogara [1] SR9011 yana hana yaduwar layin ƙwayar nono ba tare da la'akari da matsayin ER ko HER2 ba.SR9011 yana bayyana yana dakatar da zagayowar tantanin halitta na ƙwayoyin kansar nono kafin lokacin M.Cyclin A (CCNA2) an gano shi azaman jigon manufa kai tsaye na REV-ERB, yana ba da shawarar cewa hana bayyanar wannan cyclin ta SR9011 na iya yin sulhu da kama sake zagayowar tantanin halitta.Jiyya tare da SR9011 ya haifar da haɓakar ƙwayoyin cuta a cikin G0 / G1 da kuma rage yawan sel a cikin sassan S da G2 / M, suna nuna cewa kunnawa na REV-ERB na iya haifar da raguwa daga G1 zuwa S lokaci da / ko S lokaci.
Binciken Jiki:
SR9011 ya nuna madaidaicin bayyanar jini na plasma, sabili da haka, an bincika maganganun kwayoyin halittar REV-ERB a cikin hanta na berayen da aka bi da su tare da allurai daban-daban na SR9011 na kwanaki 6.Mai hana plasminogen activator nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau’in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in ƙwayar cuta (Serpine1) wani nau’in halittar REV-ERB ne na manufa kuma ya nuna matsawar magana mai dogaro da kashi a cikin martani ga SR9011.Cholesterol 7a-hydroxylase (Cyp7a1) da sterol reply element mai ɗaure furotin (Srepf1) an kuma nuna su don amsawa ga REV-ERB kuma an hana su dogaro da kashi tare da ƙara yawan SR9011.Bayan kwanaki 12 a cikin yanayin D: D, an yi allurar beraye tare da kashi ɗaya na SR9011 ko abin hawa a CT6 (mafi girman magana na Rev-erbα).Allurar mota bai haifar da rushewar ayyukan locomotor na circadian rhythmic ba.Koyaya, gudanar da kashi ɗaya na SR9011 ya haifar da asarar ayyukan locomotor yayin lokacin duhun batutuwa.Ayyuka na yau da kullun suna komawa zuwa zagaye na gaba na circadian, daidai da izinin magani na ƙasa da sa'o'i 24.A ƙarƙashin yanayin duhu akai-akai, raguwar dogaro da SR9011 a cikin halayen gudu a cikin mice ya dogara da kashi-kashi, kuma ƙarfin (ED50 = 56 mg/kg) yayi kama da na SR9011-matsakaici hanawa na reshen amsawar REV-ERB, Srebf1 , a cikin vivo (ED50 = 67mg/kg) [1].