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TSHR antagonist S37a

Names

[ CAS No. ]:
2143452-20-2

[ Name ]:
TSHR antagonist S37a

Biological Activity

[Description]:

TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy[1].

[Related Catalog]:

Research Areas >> Endocrinology
Signaling Pathways >> GPCR/G Protein >> TSH Receptor

[Target]

TSHR[1]


[In Vitro]

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[1]. 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[1].

[In Vivo]

TSHR antagonist S37a also inhibits cyclic adenosine monophosphate formation by oligoclonal TSAb, which are highly enriched in GO patients' sera[1]. TSHR antagonist S37a (10 mg/kg ;i.g.) displays no toxicity and a remarkable 53% oral bioavailability in mice[1]. Animal Model: SWISS (CD1) mice (38-43 g)[1] 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.

[References]

[1]. Marcinkowski P, et al. A New Highly Thyrotropin Receptor-Selective Small-Molecule Antagonist with Potential for the Treatment of Graves' Orbitopathy. Thyroid. 2019 Jan;29(1):111-123.

Chemical & Physical Properties

[ Molecular Formula ]:
C25H20N2O3S2

[ Molecular Weight ]:
460.57

Related Compounds