TSH Receptor Antagonist

ML224 (NCGC00242364) is a selective TSHR antagonist with an IC₅₀ value of 2.1 µM. ML224 can be used in the study of Graves' disease and other thyroid disorders.

Org 274179-0 is a low-molecular-weight allosteric thyrotropin receptor (TSH Receptor) antagonist with equipotent follicle-stimulating hormone receptor antagonistic activity and selectivity for the luteinizing hormone receptor. Org 274179-0 binds to the transmembrane domain of the thyrotropin receptor, stabilizes the receptor's inactive state, and blocks agonist-induced and constitutive signaling through the adenylyl cyclase/cAMP and phospholipase C pathways. Org 274179-0 can be used for research on Graves' disease and Graves' ophthalmopathy.

SYD5115 is an orally available TSH-R antagonist.

NCGC00229600 is an allosteric inverse agonist of thyrotropin receptor (TSHR). NCGC00229600 inhibits both TSH and stimulating antibody activation of TSHRs endogenously expressed in Graves' disease.

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

VA-K-14 hydrochloride is a specific thyroid-stimulating hormone receptor (TSHR) antagonist (IC₅₀= 12.3 μM).

Org 274178-0 is a selective thyroid-stimulating hormone receptor (TSHR) antagonist with a pIC₅₀ value for TSHR is 5.03. Org 274178-0 inhibits the activation of cAMP signaling pathway and phospholipase C (PLC) signaling pathway mediated by thyroid-stimulating hormone (TSH) and TSH receptor-stimulating immunoglobulins (TSIs). Org 274178-0 is promising for research of Graves’ disease and Graves’ ophthalmopathy.