SR1001 (SR-1001) is a novel, potent and selective antagonist/inhibitor/inverse agonist of the nuclear retinoic acid receptor-related orphan receptors RORα and RORγ with immunomodulatory effects. It inhibits RORα and RORγ with Kis 172 and 111 nM, respectively, and exhibits no activity at LXR or RORβ. RORα and RORγt are essential for the development of TH17 cells, T-helper cells that produce interleukin-17 and have recently been shown to have pathological roles in various autoimmune diseases. SR1001 binds to the ligand-binding domain of RORα and RORγt to decrease affinity of the receptor for coactivators and increse affinity for co-repressors. It inhibited the differentiation and function of TH17 cells and suppressed the clinical severity of a mouse model of multiple sclerosis.

纯度：≥98%

CAS：1335106-03-0