SYD5115 is an orally available TSH-R antagonist.
SYD5115 (0.1 nM-10 μM) blocks M22-induced cAMP production with IC50s of 22 nM in rat FRTL5 and HEK293-hTSHR cells, respectively[1] .
Note: M22 is a stimulating autoantibody to the human monoclonal TSH receptor (TSHR), and another autoantibody is K1-70 (blocking) [2].
References:
[1]. Karstens WFJ, et al. Discovery of SYD5115, a novel orally active small molecule TSH-R antagonist. Bioorg Med Chem. 2023 Apr 15;84:117258.
[2]. Furmaniak J, et al. In vivo effects of a human thyroid-stimulating monoclonal autoantibody (M22) and a human thyroid-blocking autoantibody (K1-70). Auto Immun Highlights. 2011 Sep 14;3(1):19-25.