SR1001 (1335106-03-0) is a high affinity synthetic ligand for both RORα and RORγt acting as an inverse agonist. It binds specifically to the ligand-binding domain, inducing a conformational change which leads to diminished affinity for co-activators and increased affinity for co-repressors resulting in suppression of transcriptional activity.1?SR-1001 inhibits the development of murine TH17 cells2 and suppresses the expression of cytokines1. Suppresses insulitis and prevents hyperglycemia in a type 1 diabetes mouse model.3 Protects against pathologic neovascularization in various mouse models of retinopathy.4?Active in vivo
SR 1001 is a selective RORc inverse agonist.
ChEBI: SR 1001 is a sulfonamide.
1) Solt et al. (2011) Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand; Nature, 472 491
2) Beurel et al. (2013) Inflammatory T helper 17 cells promote depression-like behavior in mice; Biol. Psychiatry, 73 622
3) Solt et al. (2015) ROR inverse agonist suppresses insulitis and prevents hyperglycemia in a mouse model of type 1 diabetes; Endocrinology, 156 869
4) Sun et al. (2015) Nuclear receptor RORα regulates pathologic retinal angiogenesis by modulating SOCS3-dependent inflammation; Proc. Natl. Acad. Sci. USA, 112 10401
