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.

SYD5115 is an orally available TSH-R antagonist.

Org 274179-0 is a potent and allosteric antagonist of thyroid-stimulating hormone (TSH) receptor, with an IC₅₀ of nanomolar concentration. Org 274179-0 completely inhibits TSH (and TSI)-mediated TSH receptor activation with little effect on the potency of TSH. Org 274179-0 can be used for the research of Graves' disease (GD).

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.