TSH Receptor

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.

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

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.

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

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.

K1-70 is a humanized antibody targeting TSHR, used in the study of autoimmune diseases and endocrine disorders.

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

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.

TSHR antagonist S37a is a selective, orally bioavailable TSHR (thyroid-stimulating hormone receptor) antagonist that inhibits TSH-induced cyclic adenosine monophosphate (cAMP) in TSHR-expressing HEK 293 cells, suitable for studying Graves' orbitopathy.

Pentacosafluorotridecanoic Acid (PFTrDA) is a perfluoroalkyl substance (PFAS) that exhibits various biological impacts across different species. In zebrafish embryos, exposure to PFTrDA induces yolk sac edema and increases mRNA expression of thyroid hormone synthesis genes, including tshβ, at concentrations of 0.1 and 0.3 mg/L. At a dosage of 10 mg/kg, PFTrDA reduces serum testosterone and luteinizing hormone levels, as well as palmitic acid, linoleic acid, and oleic acid levels in the testicular interstitial cells of late adolescent rats. In humans, maternal plasma levels of PFTrDA during pregnancy are positively correlated with the development of eczema in female infants (but not male infants), and PFTrDA levels are higher in the livers of cancerous humans compared to non-cancerous ones. Additionally, PFTrDA is found in marine mammals.

Thyrotropin (TSH), a thyroid-stimulating hormone, is synthesized by thyrotrope cells in the anterior pituitary gland and modulates the endocrine activity of the thyroid [1] [2].

MS438 is an effective agonist of the TSH receptor.

SYD5115 is an orally active TSH-R antagonist.

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.

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).

PGlu-3-methyl-His-Pro-NH2 TFA enhances binding to pituitary TRH receptors, thereby increasing the stimulation of thyroid-stimulating hormone (TSH) release from the pituitary.

Anti-TSHR Antibody (M22) is a humanized IgG1 monoclonal antibody targeting the thyroid-stimulating hormone receptor (TSHR). This antibody is capable of inhibiting the interaction between TSH and TSHR.

TSHR antagonist S37b, the less potent enantiomer of TSHR antagonist S37a, exhibits minimal efficacy in inhibiting the thyrotropin receptor (TSHR). It is utilized in thyroid function research[1].

MS437 is a potent TSH receptor agonist.