graves' disease

Carbimazole (Athyromazole) is an Imidazolium thyroid antagonist, which is rapidly transformed into MMI in vivo and can be converted into methidazole in vitro, and can be used in the study of Graves' disease.

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.

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

Org 274179-0 is an effective allosteric antagonist of the thyroid-stimulating hormone (TSH) receptor, with an IC50 in the nanomolar range. It fully inhibits TSH (and TSI)-mediated activation of the TSH receptor with minimal impact on the efficacy of TSH. This compound can be utilized in studies of Graves' disease (GD).

TR antagonist 2 (Compound 10a) is a competitive inhibitor of thyroid hormone receptors (TRα/β) with an IC50 of 47 nM. It works by competitively binding to the ligand-binding domain of the receptor with triiodothyronine (T3), thereby blocking the formation of the receptor-coactivator complex, inhibiting target gene transcription, and reducing thyroid hormone-mediated metabolic effects. TR antagonist 2 holds potential for research into hyperthyroidism (such as Graves' disease) and thyrotoxicosis.

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

Benzylthiouracil (6-Benzyl-2-thiouracil) induces ANCA-associated glomerulonephritis in Graves' disease patients and is used to study hyperthyroidism.

VRDN-002 is a humanized monoclonal antibody (mAb) targeting IGF1R/CD221. It is designed to reduce inflammation and exophthalmos associated with thyroid eye disease (TED). Additionally, VPI-2690B is utilized in research related to Graves' ophthalmopathy.