TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy.
IC50&Target
TSHR
体外研究
TSHR antagonist S37a exhibits inhibition activity for TSHR, with IC50s of 40 µM and approximately 20 µM 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.
体内研究
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.
Animal Model:
SWISS (CD1) mice (38-43 g)
Dosage:
10 mg/kg
Administration:
Oral gavage
Result:
Displays a remarkable 53% oral bioavailability as well as a half‐life of 2.9 hours after oral application.
分子式
C25H20N2O3S2
分子量
460.57
CAS号
2143452-20-2
运输条件
Room temperature in continental US; may vary elsewhere.