Tshuag API Raw Khoom Pharma Qib Siab Zoo SR9011 CAS 1379686-29-9 Rau Lub Cev Muaj Zog
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Kev siv
SR9011 yog REV-ERBα / β agonist nrog IC50s ntawm 790 nM thiab 560 nM rau REV-ERBα thiab REV-ERBβ, feem.Yuav kho mob qog noj ntshav.
Myocardial infarction yog ib qho ntawm cov kab mob uas muaj kev tuag ntau tshaj plaws ntawm cov kab mob plawv.Myocardial infarction yog tshwm sim los ntawm coronary artery stenosis los yog spasm, ua rau mob los yog tsis tu ncua myocardial ischemia thiab hypoxia, thiab myocardial cell tuag.Ntau yam pro-inflammatory cytokines xws li interleukin-1β (IL-1β) thiab qog necrosis factor-α (TNF-α) koom nrog hauv myocardial remodeling3.SR9011 yog REV-ERBα / β agonist, ib tug tswv cuab ntawm tsev neeg ntawm cov receptor nuclear, thiab cov kev tshawb fawb tau pom tias nws tuaj yeem tswj cov metabolism hauv cov nqaij mos.Huang Guodong pom tias SR9011 ua lub luag haujlwm tseem ceeb hauv kev tswj cov kab mob autophagy noob hauv zebrafish.
C-terminus ntawm SR9011 tsev neeg cov protein tsis muaj ligand-binding domain, tab sis nws muaj peev xwm inhibit qhov kev qhia ntawm Rev-erb protein los ntawm recruiting nuclear receptor repressor factor thiab histone deacetylase 3, thiab lwm yam. Histone deacetylase 3 yog Rev-erb agonist thiab ib tug me me molecule tshuaj soj ntsuam.Fon-taine thawj zaug tshaj tawm hauv Chemicalbook tias muaj kev sib raug zoo ntawm SR9011 thiab o, thiab SR9011 tuaj yeem cuam tshuam qhov kev qhia ntawm Tr4, yog li tswj cov teeb liab inflammatory.Cov kws tshawb fawb txawv teb chaws tau pom tias nyob rau hauv tib neeg macrophages, nce mRNA qhia ntawm SR9011 los ntawm cov kws tshuaj ncaj qha ua rau txo qis hauv mRNA qhia ntawm pro-inflammatory yam cuam tshuam interleukin-6.
Synonymous:
| 1-Pyrrolidinecarboxamide, 3-[[[(4-chlorophenyl)methyl][(5-nitro-2-thienyl)methyl]amino]methyl]-N-pentyl- |
| TIAB SA 9011 |
| UNII: VYI79FLZ6W |
| 3-({(4-Chlorobenzyl)[(5-nitro-2-thienyl)methyl]amino}methyl)-N-pentyl-1-pyrrolidinecarboxamide |
SR9011 CAS 1379686-29-9 Kev Tshawb Fawb:
Kev tshawb nrhiav hauv vitro:
SR9011 dose-dependently nce REV-ERB-dependent repressor kev ua haujlwm thiab RE4- Tus neeg saib xyuas luciferase (REV-ERBα IC50 = 790 nM, REV-ERBβ IC50 = 560 nM).SR9011 muaj zog thiab muaj peev xwm txwv tsis pub hloov pauv hauv kev sib koom ua ke kev sib txuas nrog kev siv tag nrho REV-ERBα nrog rau cov neeg sau xov xwm luciferase gene uas tau tsav los ntawm Bmal1 txhawb nqa (SR9011 IC50 = 620nM).SR9011 inhibits BGAL1 mRNA kev qhia hauv HepG2 hlwb hauv REV-ERBα / beta-dependent yam[1] SR9011 inhibits kev loj hlob ntawm cov kab mob qog noj ntshav mis tsis hais lawv ER lossis HER2 li cas.SR9011 zoo nkaus li nres lub voj voog ntawm cov qog nqaij hlav cancer ntawm lub mis ua ntej M theem.Cyclin A (CCNA2) tau txheeb xyuas tias yog lub hom phiaj ncaj qha ntawm REV-ERB, qhia tias inhibition ntawm qhov kev qhia ntawm no cyclin los ntawm SR9011 tuaj yeem kho lub voj voog ntawm tes.Kev kho mob nrog SR9011 ua rau cov hlwb nce ntxiv hauv G0 / G1 theem thiab txo cov hlwb hauv S thiab G2 / M theem, qhia tias kev ua kom REV-ERB tuaj yeem ua rau txo qis ntawm G1 mus rau S theem thiab / lossis S theem.
Kev tshawb fawb lub cev:
SR9011 tau pom tias tsim nyog rau cov ntshav plasma, yog li ntawd, qhov kev qhia ntawm REV-ERB teb cov noob tau tshuaj xyuas hauv daim siab ntawm cov nas uas tau kho nrog ntau koob tshuaj SR9011 rau 6 hnub.Lub plasminogen activator inhibitor hom 1 noob (Serpine1) yog REV-ERB lub hom phiaj gene thiab pom cov koob tshuaj tiv thaiv kev tawm tsam hauv kev teb rau SR9011.Cov roj (cholesterol) 7α-hydroxylase (Cyp7a1) thiab sterol teb cov ntsiab lus khi cov protein (Srepf1) noob kuj tau pom tias yuav teb rau REV-ERB thiab tau txhaj tshuaj raws li inhibited nrog nce ntxiv ntawm SR9011.Tom qab 12 hnub hauv D: D, cov nas tau txhaj tshuaj ib zaug ntawm SR9011 lossis lub tsheb ntawm CT6 (qhov siab tshaj plaws ntawm Rev-erbα).Kev txhaj tshuaj tsheb tsis ua rau muaj kev cuam tshuam ntawm circadian rhythmic locomotor kev ua haujlwm.Txawm li cas los xij, kev tswj hwm ntawm ib koob tshuaj ntawm SR9011 ua rau poob ntawm kev ua haujlwm hauv lub cev thaum lub sijhawm tsaus ntuj.Kev ua haujlwm ib txwm rov qab mus rau lub voj voog circadian tom ntej, zoo ib yam nrog cov tshuaj tshem tawm tsawg dua 24 teev.Nyob rau hauv qhov tsaus ntuj tsis tu ncua, SR9011-raws li kev txo qis hauv kev coj tus cwj pwm hauv cov nas yog nyob ntawm koob tshuaj, thiab lub zog (ED50 = 56 mg / kg) zoo ib yam li SR9011-mediated inhibition ntawm REV-ERB teb cov noob, Srebf1 , in vivo (ED50 = 67mg/kg) [1].