1335106-03-0
1335106-03-0 结构式
基本信息
SR-1001
SR 1001
SR1001 >=98% (HPLC)
N-(5-(N-(4-(1,1,1,3,3,3-Hexafluoro-2-hydroxypropan-2-yl)phenyl)sulphamoyl)-4-methylthiazol-2-yl)acetamide
N-(5-{[4-(1,1,1,3,3,3-Hexafluoro-2-hydroxy-2-propanyl)phenyl]sulfamoyl}-4-methyl-1,3-thiazol-2-yl)acetamide
N-[4-Methyl-5-[[[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]amino]sulfonyl]-2-thiazolylacetamide
SR1001,N-{4-Methyl-5-[4-(2,2,2-trifluoro-1-hydroxy-1-trifluoroMethyl-ethyl)-phenylsulfaMoyl]-thiazol-2-yl}-acetaMide
Acetamide, N-[4-methyl-5-[[[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]amino]sulfonyl]-2-thiazolyl]-
物理化学性质
常见问题列表
| Target | Value |
|
RORγ
() | 111 nM(Ki) |
|
RORα
() | 172 nM(Ki) |
SR1001 inhibits the development of murine T H 17 cells by inhibition of IL-17A gene expression and protein production. SR1001 reduces the interaction of a coactivator TRAP220 NR box 2 peptide with ROR γ in a dose dependent manner (IC 50 value≈117 nM). Additionally, SR1001 inhibits the expression of cytokines when added to differentiated murine or human T H 17 cells.
SR1001 effectively suppresses the clinical severity of autoimmune disease in mice. Administration of SR1001 to C57BL/6 mice suppresses the expression of hepatic ROR target genes, Cyp7b1, Rev-erbα, and Serpine 1. SR1001 a ROR α inverse agonist eliminats the circadian pattern of expression of citrate synthase mRNA in mice.