SR 1555 (hydrochloride) |
Catalog No.GC14418 |
inverse agonist of RORγ
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
SR 1555 is a novel RORγ-specific synthetic ligand [1].
Retinoic acid receptor-related nuclear receptor (ROR) belongs to the nuclear receptor superfamily, a group of structurally related, ligand-dependent transcription factors. RORs function as key regulators of many physiological processes that occur during embryonic development and in the adult [2]. RORγ plays a dominant role in T cell differentiation, particularly in the development of TH17 cells, which are implicated in autoimmune diseases such as multiple sclerosis and rheumatoid arthritis [3].
In vitro: In a GAL4-NR chimeric co-transfection assay, SR1555 was devoid of LXR, FXR, and RORα activity, but it dose-dependently repressed the activity at RORγ with an IC50 of ≈ 1.5 μM. In competitive radioligand binding assays, SR1555 bound to RORγ with an IC50 of 1 μM. SR1555 specifically targeted RORγ and inhibited its transcriptional activity leading to suppression of IL-17 gene expression. EL4 cells treated SR1555 (10 μM) for 24 h inhibited Il17a gene expression by greater than 70%, demonstrating that SR1555 could inhibit the expression of this TH17 mediated cytokine [1]. SR1555 not only inhibited TH17 cell development and function but also increased the frequency of T regulatory cells [1].
References:
[1] Solt L A, Kumar N, He Y, et al. Identification of a selective RORγ ligand that suppresses Th17 cells and stimulates T regulatory cells[J]. ACS chemical biology, 2012, 7(9): 1515-1519.
[2] Jetten A M, Ueda E. The ROR nuclear orphan receptor subfamily: critical regulators of multiple biological processes[J]. Progress in nucleic acid research and molecular biology, 2001, 69: 205-247.
[3] Ivanov I I, McKenzie B S, Zhou L, et al. The orphan nuclear receptor RORγt directs the differentiation program of proinflammatory IL-17+ T helper cells[J]. Cell, 2006, 126(6): 1121-1133.
Average Rating: 5
(Based on Reviews and 11 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *