Biological Activity
TSHR antagonist S37 is a selective and competitive antagonist of the thyrotropin receptor (TSHR).
TSHR antagonist S37 not only inhibits the thyrotropin receptor (TSHR) activation by thyrotropin itself but also activation by monoclonal TSAb M22 (human), KSAb1 (murine), and the allosteric small-molecule agonist C2. Disease-related ex vivo studies in HEK 293 cells expressing the TSHR shows that TSHR antagonist S37 also inhibits cyclic adenosine monophosphate formation by oligoclonal thyroid stimulating antibodies (TSAb).[1]
TSHR antagonist S37 has no toxicity and a remarkable 53% oral bioavailability in mice, indicating by initial in vivo pharmacokinetic studies.[1];
