TSHR antagonist S37a

TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy In Vitro TSHR antagonist S37a exhibits inhibition activity for TSHR, with IC 50 s 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. IC50& Target:TSHR

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