SR 1001 |
| Catalog No.GC15009 |
SR 1001 est un agoniste inverse sélectif RORα et RORγt avec Kis 172 et 111 nM, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1335106-03-0
Sample solution is provided at 25 µL, 10mM.
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SR1001 is a selective RORα and RORγ inverse agonist with Kis 172 and 111 nM, respectively.
SR1001 inhibits the development of murine TH17 cells by inhibition of IL-17A gene expression and protein production. SR1001 reduces the interaction of a coactivator TRAP220 NR box 2 peptide with RORγ in a dose dependent manner (IC50 value≈117 nM). Additionally, SR1001 inhibits the expression of cytokines when added to differentiated murine or human TH17 cells[1].
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[1]. SR1001 a RORα inverse agonist eliminats the circadian pattern of expression of citrate synthase mRNA in mice[2].
References:
[1]. Solt LA, et al. Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand. Nature. 2011 Apr 28;472(7344):491-4.
[2]. Crumbley C, et al. Regulation of expression of citrate synthase by the retinoic acid receptor-related orphan receptor α (RORα). PLoS One. 2012;7(4):e33804.
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