SR1001|SR-1001,SR 1001|DC Chemicals
SR1001 is a high-affinity synthetic ligand of RORα and RORγ; suppresses TH17 cell differentiation and inhibits autoimmunity.
Catlog: DC8096| Product name: SR1001| Cas: 1335106-03-0| Other names: SR-1001,SR 1001| Molecule Formula: C15H13F6N3O4S2| MW: 477.4. Purity: >98%
Price: 100mg: 600 USD; 250mg: 1100 USD; 1000mg: 1950 USD
SR1001 is a high-affinity synthetic ligand of RORα and RORγ; suppresses TH17 cell differentiation and inhibits autoimmunity.
in vitro: SR1001 binds specifically to the ligand-binding domains of RORα and RORγt, inducing a conformational change within the ligand-binding domain that encompasses the repositioning of helix 12 and leads to diminished affinity for co-activators and increased affinity for co-repressors, resulting in suppression of the receptors' transcriptional activity. SR1001 inhibited the development of murine T(H)17 cells, as demonstrated by inhibition of interleukin-17A gene expression and protein production. Furthermore, SR1001 inhibited the expression of cytokines when added to differentiated murine or human T(H)17 cells. SR1001 reduced the interaction of a coactivator TRAP220 NR box 2 peptide with RORγ in a dose dependent manner(IC50=117 nM).
in vivo: SR1001 was a RORα inverse agonist eliminated the circadian pattern of expression of CS mRNA in mice.
For research and scientific purpose only, not for human use.
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