TSH Receptor

ML224 (NCGC00242364) is a TSHR antagonist for the treatment of Graves' orbital disease and Graves' hyperthyroidism.

ML-109 is a potent agonist of thyroid stimulating hormone receptor (TSHR) (EC50 of 40 nM)

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

Org41841 is an agonist of luteinising hormone/chorionic gonadotropin receptor and thyroid stimulating hormone receptor (EC50s: 0.2 and 7.7 μM, respectively) and can be used to study hyperthyroidism.

TSHR antagonist S37 is a selective and competitive antagonist of the thyrotropin receptor (TSHR).

VA-K-14 hydrochloride（VAK14 HCl） is a selective thyrotropin receptor (TSHR) antagonist (IC50= 12.3 μM) that inhibits TSHR stimulation by serum and monoclonal TSHR-stimulating antibodies from patients with GD and abrogates TSHR signaling.

D3-βArr (NCGC00379308) is a positive allosteric modulator for thyrotropin receptor (TSHR), which initiates translocation of β-Arr 1 (EC50: 11.6 μM) by direct TSHR activation.

Teprotumumab is a human monoclonal antibody that blocks the IGF-1 receptor (IGF-1R). Teprotumumab binds to the extracellular α-subunit domain ligand of IGF-1R. Teprotumumab inhibits TSH and IGF-1 action in fibrocytes. Teprotumumab reduces TSH-dependent IL-6 and IL-8 expression and Akt phosphorylation. Teprotumumab can be used in the study of thyroid-associated eye diseases.

NCATS-SM4420 (Compound A35) is an orally effective ligand for the thyroid-stimulating hormone receptor (TSHR) that inhibits the proliferation of MDA-T32 and MDA-T85 cells both in vitro and in vivo, with IC50 values of 0.71 μM and 0.38 μM, respectively. Additionally, it suppresses the metastasis of MDA-T85F1 in mice. NCATS-SM4420 holds potential for research in the field of thyroid cancer.