Kūʻai API Raw Material Pharma Grade High Quality SR9011 CAS 1379686-29-9 No ke kino
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Hoʻohana
ʻO SR9011 he REV-ERBα / β agonist me IC50s o 790 nM a me 560 nM no REV-ERBα a me REV-ERBβ, kēlā me kēia.Hiki ke mālama i ke kanesa.
ʻO ka myocardial infarction kekahi o nā maʻi me ka nui o ka make o nā maʻi cardiovascular.Hoʻokumu ʻia ka myocardial infarction ma muli o ka stenosis coronary artery a i ʻole spasm, ka hopena o ka ischemia myocardial a me ka hypoxia, a me ka make o ka myocardial cell.ʻO nā cytokine pro-inflammatory like ʻole e like me interleukin-1β (IL-1β) a me ka tumor necrosis factor-α (TNF-α) i komo i ka hoʻoponopono hou ʻana o ka myocardial3.ʻO SR9011 he REV-ERBα / β agonist, he lālā o ka ʻohana nuklear receptor, a ua ʻike nā haʻawina hiki iā ia ke hoʻoponopono i ka metabolism o nā mea olaola.Ua ʻike ʻo Huang Guodong he kuleana koʻikoʻi ka SR9011 i ka hoʻoponopono ʻana i ke kani o nā genes autophagy i ka zebrafish.
ʻO ka C-terminus o ka protein ʻohana SR9011 ʻaʻole i loaʻa kahi ligand-binding domain, akā hiki iā ia ke kāohi i ka hōʻike ʻana o Rev-erb protein ma o ka hoʻopaʻa ʻana i ka mea hoʻopiʻi nuklear receptor repressor factor a me ka histone deacetylase 3, etc. ʻO Histone deacetylase 3 he Rev-erb agonist a he ʻimi kinikini liʻiliʻi.Ua hōʻike mua ʻia ʻo Fon-taine ma Chemicalbook aia kahi pilina ma waena o SR9011 a me ka mumū, a hiki i ka SR9011 ke kāohi i ka hōʻike ʻana o Tr4, a laila e hoʻomalu i ka hōʻailona inflammatory.Ua ʻike nā haumāna haole i loko o nā macrophages kanaka, hoʻonui i ka hōʻike mRNA o SR9011 e nā ʻano pharmacological e alakaʻi pololei i ka emi ʻana o ka hōʻike mRNA o ka mea pro-inflammatory interleukin-6.
Kaulike:
| 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 Noiʻi:
Ka noiʻi in vitro:
SR9011 dose-dependently hoʻonui REV-ERB-dependent repressor hana a me RE4- Responsive luciferase reporter (REV-ERBα IC50 = 790 nM, REV-ERBβ IC50 = 560 nM).Hoʻopiʻi ikaika ʻo SR9011 i ka transcription ma kahi hoʻololi co-transfection assay me ka hoʻohana ʻana i ka REV-ERBα holoʻokoʻa me kahi ʻano mea hoʻolaha luciferase i alakaʻi ʻia e ka mea hoʻolaha Bmal1 (SR9011 IC50 = 620nM).Hoʻopili ʻo SR9011 i ka hōʻike BGAL1 mRNA i nā cell HepG2 ma kahi REV-ERBα/β-dependence [1] SR9011 inhibits the proliferation of breast cancer cell lines inquiry their ER or HER2 status.ʻIke ʻia ʻo SR9011 e hoʻomaha i ka pōʻai cell o nā maʻi maʻi maʻi umauma ma mua o ka M phase.Ua ʻike ʻia ʻo Cyclin A (CCNA2) ma ke ʻano he kumu kuhikuhi pololei o REV-ERB, e hōʻike ana i ka hoʻopaʻa ʻana i ka hōʻike ʻana o kēia cyclin e SR9011 hiki ke hoʻopaʻa i ka hopu ʻana i ke kelepona.ʻO ka hoʻomaʻamaʻa ʻana me SR9011 ka hopena i ka hoʻonui ʻia ʻana o nā cell i ka pae G0/G1 a me ka hoʻemi ʻana o nā cell i nā ʻāpana S a me G2/M, e hōʻike ana i ka hoʻoulu ʻana o REV-ERB hiki ke hopena i kahi hoʻololi hoʻemi mai ka pae G1 a i ka pae S a i ʻole ka pae S.
Ka noiʻi kino:
Ua hōʻike ʻo SR9011 i ka hōʻike plasma kūpono, no laila, ua nānā ʻia ka ʻōlelo o REV-ERB pane pane i loko o nā ate o nā ʻiole i mālama ʻia me nā ʻano like ʻole o SR9011 no nā lā 6.ʻO ka plasminogen activator inhibitor type 1 gene (Serpine1) he REV-ERB target gene a hōʻike i ka hoʻopaʻa ʻana i ka hopena o ka hōʻike i ka pane ʻana iā SR9011.Ua hōʻike pū ʻia nā genes Cholesterol 7α-hydroxylase (Cyp7a1) a me ka sterol response element binding protein (Srepf1) e pane i REV-ERB a ua hoʻopaʻa ʻia i ka nui o ka SR9011.Ma hope o nā lā 12 i nā kūlana D: D, ua hoʻopiʻi ʻia nā ʻiole me kahi pā hoʻokahi o SR9011 a i ʻole kaʻa ma CT6 (hōʻike kiʻekiʻe o Rev-erbα).ʻAʻole i hoʻopilikia ʻia ka hana circadian rhythmic locomotor kaʻa kaʻa.Eia nō naʻe, ʻo ka hoʻokele ʻana i hoʻokahi dosis o SR9011 i hopena i ka nalowale o ka hana locomotor i ka wā pōʻeleʻele o nā kumuhana.Hoʻi ka hana maʻamau i ka pōʻai circadian aʻe, e like me ka hoʻomaʻemaʻe lāʻau ma lalo o 24 mau hola.Ma lalo o nā kūlana pōʻeleʻele mau, ʻo ka SR9011 i hilinaʻi ʻia i ka holo ʻana o ka huila i nā ʻiole i hilinaʻi ʻia, a ua like ka mana (ED50 = 56 mg / kg) me ka SR9011-mediated inhibition o ka REV-ERB pane pane, Srebf1 , in vivo (ED50 = 67mg/kg) [1].