Stock API Raw Material Pharma Grade High Quality SR9011 CAS 1379686-29-9
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Consuetudinem
SR9011 est agonista REV-ERBα/β cum IC50s 790 nM et 560 nm pro REV-ERBα et REV-ERBβ, respective.Potest cancer tractare.
Infarctio myocardialis una est e morbis cum summa mortalitatis rate in morbis cardiovascularibus.Infarctio myocardialis causatur ex arteria coronaria stenosis vel distentione nervorum, inde in ischemia et hypoxia myocardiali vel pervicax, et mors cellula myocardialis.Variae cytokinae pro-inflammatoriae ut interleukin-1β (IL-1β) et tumor necrosis factoris-α (TNF-α) implicantur in revellere myocardiali.SR9011 est REV-ERBα/β agonist, membrum receptoris familiae nuclei, et studia invenerunt eum metabolismi textuum biologicorum moderari posse.Huang Guodong invenit SR9011 munus magni momenti esse in moderandis genesis autophagiae in zebrafish.
C-terminum familiae SR9011 dapibus ligandi vinculo regio caret, sed expressionem Rev-erb interdum inhibere factorem repressoris nuclei et histonii deacetylasii 3, etc. Histon deacetylasius 3 est Rev-erb agonist ac a parva moleculae chemicae specillo.Fon-taine primum in Chemicalbook nuntiavit relationem esse inter SR9011 et inflammationem, et SR9011 expressionem Tr4 inhibere potest, eoque signo inflammationis moderante.Externi scholares invenerunt quod in macrophages humana, crescens modus expressionis SR9011 per methodos pharmacologicos directe ad diminutionem in expressione variantis factoris pro-inflammatorii interleukin-6.
Synonyma
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 Research:
In vitro investigationis
SR9011 dosis dependenter auctus REV-ERB-repressor actio dependens et RE4- notario responsiva luciferae (REV-ERBα IC50 = 790 nM, REV-ERBβ IC50 = 560 nM).SR9011 potenter et potenter transcriptionem reprimit in co-perductione intenta utens plena longitudine REV-ERBα cum notario generum luciferasi a promotore Bmal1 agitato (SR9011 IC50 = 620nM).SR9011 vetat BGAL1 mRNA expressio in cellulis HepG2 in modo REV-ERBα/β-dependens [1] SR9011 vetat multiplicationem linearum cancri pectoris, cujuscumque status eorum ER vel HER2.SR9011 morare videtur cellulae cycli carcinomatis carcinomatis ante M Phase.Cyclin A (CCNA2) quasi signum directum gene of REV-ERB notum est, suggerens inhibitionem expressionis huius cyclini per SR9011 comprehendi posse mediare cyclum cellularum.Curatio cum SR9011 consecuta est in cellulis auctis in G0/G1 periodo et cellulis in S et G2/M decrescentibus, suggerens ut activatio REV-ERB inveniatur in diminuto transitu ab G1 ad S periodo et/vel S periodo.
Physica investigationis
SR9011 rationabilem expositionem plasma demonstravit, expressio genesis REV-ERB responsabilis examinata est in iecore murium cum diversis bibulis SR9011 per 6 dies tractata.Plasminogen activator inhibitoris generis 1 gene (Serpine1) est scopum REV-ERB gene et dosis dependens repressionem expressionis in responsione ad SR9011 ostendit.Cura 7α-hydroxylase (Cyp7a1) et steroli responsionis elementi ligaturae interdum (Srepf1) genes ostensae sunt etiam ut REV-ERB responderent et doses dependenter inhibitae cum copia SR9011 augerentur.Post 12 dies in D:D conditiones, mures cum uno pondere SR9011 vel vehiculi CT6 injecti sunt (apicem expressionis Rev-erbα).Vehiculum injectiones non evenerunt in distractis actionis locomotoris rhythmicae circadianae.Attamen administratio unius dosis SR9011 consecuta est in detrimento actionis locomotoriae in tenebris phase subditorum.Normalis operatio ad cyclum circadianum proximum redit, quod medicamentis alvi minus quam 24 horis convenit.Sub constantibus atris condicionibus, reductione SR9011-dependens in rotae currendo mores in muribus dosis dependens erat, et potentia (ED50 = 56 mg/kg) similis erat cum inhibitione responsionis SR9011 mediatae gene, Srebf1 REV-ERB. , in vivo (ED50 = 67mg/kg) [1].