TSHR antagonist S37a

2143452-20-2

460.57

10 mM in DMSO

GPCR/G Protein

TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy.
IC50 & Target: TSHR
In Vitro: TSHR antagonist S37a exhibits inhibition activity for TSHR, with IC50s of 40 uM and approximately 20 uM for mTSHR and hTSHR, respectively, in HEK293 cells.

TSHR antagonist S37a not only inhibits the TSHR activation by thyrotropin itself but also activation by monoclonal TSAb M22 (human), KSAb1 (murine), and the allosteric small-molecule agonist C2.

In Vivo: TSHR antagonist S37a also inhibits cyclic adenosine monophosphate formation by oligoclonal TSAb, which are highly enriched in GO patients' sera.

TSHR antagonist S37a (10 mg/kg ; i.g.) displays no toxicity and a remarkable 53% oral bioavailability in mice.