Ngwaahịa API Raw Material Pharma ọkwa dị elu SR9011 CAS 1379686-29-9 Maka Mwube ahụ
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SR9011 bụ REV-ERBα/β agonist nwere IC50s nke 790 nM na 560 nM maka REV-ERBα na REV-ERBβ, n'otu n'otu.Nwere ike ịgwọ ọrịa kansa.
Myocardial infarction bụ otu n'ime ọrịa ndị nwere ọnụ ọgụgụ kachasị elu nke ọrịa obi na-anwụ.Myocardial infarction na-akpata site na akwara akwara obi stenosis ma ọ bụ spasm, na-ebute nnukwu ma ọ bụ na-adịgide adịgide myocardial ischemia na hypoxia, na ọnwụ cell myocardial.Cytokines pro-inflammatory dị iche iche dị ka interleukin-1β (IL-1β) na tumor necrosis factor-α (TNF-α) na-etinye aka na nhazigharị myocardial3.SR9011 bụ REV-ERBα/β agonist, onye so na ezinụlọ nnata nuklia, na ọmụmụ achọpụtala na ọ nwere ike ịhazi metabolism nke anụ ahụ dị ndụ.Huang Guodong chọpụtara na SR9011 na-arụ ọrụ dị mkpa n'ịchịkwa ụda nke mkpụrụ ndụ ihe nketa autophagy na zebrafish.
C-terminus nke protein ezinụlọ SR9011 enweghị ngalaba njikọ njikọ, mana ọ nwere ike igbochi nkwupụta nke protein Rev-erb site n'iweta ihe na-anabata ihe na-anabata ihe na histone deacetylase 3, wdg. Histone deacetylase 3 bụ Rev-erb agonist na obere nyocha kemịkalụ molekul.Fon-taine buru ụzọ kọọ na Chemicalbook na enwere njikọ dị n'etiti SR9011 na mbufụt, yana SR9011 nwere ike igbochi okwu Tr4, si otú ahụ na-achịkwa mgbama mkpali.Ndị ọkà mmụta si mba ọzọ achọpụtala na na macrophages mmadụ, ịba ụba okwu mRNA nke SR9011 site na usoro ọgwụ na-eduga ozugbo na mbelata okwu mRNA nke pro-inflammatory factor interleukin-6.
Oyiri:
| 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 |
Nyocha SR9011 CAS 1379686-29-9:
Nnyocha in vitro:
SR9011 dose-dabere na-abawanye ọrụ repressor na-adabere na REV-ERB na RE4-Responsive luciferase reporter (REV-ERBα IC50 = 790 nM, REV-ERBβ IC50 = 560 nM).SR9011 na-eji ike na-eji ike na-ejigide ederede na nyocha mmekọ mgbanwe site na iji REV-ERBα zuru oke yana mkpụrụ ndụ nta akụkọ luciferase nke onye nkwalite Bmal1 na-ebugharị (SR9011 IC50 = 620nM).SR9011 na-egbochi okwu BGAL1 mRNA na mkpụrụ ndụ HepG2 n'ụzọ REV-ERBa/β-dabere[1] SR9011 na-egbochi mmụba nke ahịrị mkpụrụ ndụ kansa ara n'agbanyeghị ọkwa ER ma ọ bụ HER2 ha.SR9011 dị ka ọ na-akwụsịtụ usoro mkpụrụ ndụ kansa ara tupu oge M.Achọpụtara Cyclin A (CCNA2) dị ka mkpụrụ ndụ ebumnuche ebumnuche kpọmkwem nke REV-ERB, na-atụ aro na mgbochi nke okwu cyclin a site na SR9011 nwere ike mebie njide okirikiri cell.Ọgwụgwọ na SR9011 mere ka mkpụrụ ndụ mụbaa na mpaghara G0/G1 ma belata mkpụrụ ndụ na akụkụ S na G2 / M, na-atụ aro na ịgbalite REV-ERB nwere ike ime ka mbelata mgbanwe site na G1 ruo S na / ma ọ bụ S.
Nnyocha anụ ahụ:
SR9011 gosipụtara ngosipụta plasma ezi uche dị na ya, ya mere, a na-enyocha ngosipụta nke mkpụrụ ndụ ihe nketa REV-ERB n'ime imeju ụmụ oke ejiri ọgwụ dị iche iche nke SR9011 mee ihe maka ụbọchị 6.Ụdị 1 ụdị plasminogen activator inhibitor (Serpine1) bụ mkpụrụ ndụ ihe mgbaru ọsọ REV-ERB ma gosipụta mmegide okwu dabere na dose na nzaghachi SR9011.Cholesterol 7a-hydroxylase (Cyp7a1) na sterol nzaghachi ihe na-ejikọta protein (Srepf1) mkpụrụ ndụ ihe nketa gosikwara ka ha zaghachi REV-ERB ma na-egbochi dose-dabere na ọnụ ọgụgụ SR9011 na-abawanye.Mgbe ụbọchị 12 gasịrị na ọnọdụ D: D, a na-agbanye ụmụ oke na otu dose nke SR9011 ma ọ bụ ụgbọ ala na CT6 (okwu kachasị elu nke Rev-erbα).Ịgba ntụtụ ụgbọ ala ebuteghị nkwụsị nke ọrụ locomotor rhythmic circadian.Agbanyeghị, nchịkwa otu dose nke SR9011 butere mfu nke ọrụ locomotor n'oge oge ọchịchịrị nke isiokwu ndị ahụ.Ọrụ nkịtị na-alaghachi na okirikiri circadian na-esote, kwekọrọ na mkpochapụ ọgwụ na-erughị awa 24.N'okpuru ọnọdụ gbara ọchịchịrị mgbe niile, mbelata SR9011 na-adabere na omume ịgba ọsọ wheel na ụmụ oke na-adabere na dose, na ike (ED50 = 56 mg/kg) yiri nke SR9011-mediated mgbochi nke REV-ERB nzaghachi gene, Srebf1. , na vivo (ED50 = 67mg/kg) [1].