2. Signaling Pathways
  3. GPCR/G Protein
  4. TSH Receptor

TSH Receptor

Thyrotropin receptor; Thyroid-stimulating hormone Receptor

TSH Receptor

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The TSH receptor (TSHR) is a member of the glycoprotein hormone receptors, a subfamily of family A G protein-coupled receptors. The TSH receptor (TSHR) undergoes complex post –translational modifications including intramolecular cleavage and receptor multimerization. TSHR and its endogenous ligand thyrotropin (TSH) are of essential importance for growth and function of the thyroid gland and proper function of the TSH/TSHR system is pivotal for production and release of thyroid hormones.

The TSHR activates different G-protein subtypes and signaling pathways, whereby Gs- and Gq-induced signaling are probably of highest importance. TSH and its receptor are required for thyroid hormone synthesis and release in the thyroid gland. Dysfunctions of the TSHR are the underlying cause of various gain- or loss-of-function phenotypes associated with thyroid malfunction. It has been suggested that the TSHR is involved in the development and mechanisms of ophthalmopathy. TSHR is also a major autoantigen for autoimmune diseases of the thyroid gland. In addition, TSHR has been proposed to be a potent target against thyroid cancer with several experimental compounds under development.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-12381
    ML224
    		Antagonist 99.18%
    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.
    ML224
  • HY-P99165
    Teprotumumab
    		Inhibitor 99.46%
    Teprotumumab is an IGF-1 receptor (IGF-1R) blocking human monoclonal antibody. Teprotumumab binds to the ligand binding extracellular α-subunit domain of IGF-1R. Teprotumumab inhibits TSH and IGF-1 action in fibrocytes. Teprotumumab attenuates TSH-dependent IL-6 and IL-8 expression and Akt phosphorylation. Teprotumumab can be used for thyroid-associated ophthalmopathy research.
    Teprotumumab
  • HY-114116
    ML-109
    		Agonist 99.12%
    ML-109 is a potent and full thyroid stimulating hormone receptor (TSHR) agonist, with an EC50 of 40 nM.
    ML-109
  • HY-129995A
    TSHR antagonist S37a
    		Antagonist 98.00%
    TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy.
    TSHR antagonist S37a
  • HY-158100
    SYD5115
    		Antagonist 99.69%
    SYD5115 is an orally available TSH-R antagonist.
    SYD5115
  • HY-114994
    MS437
    		Activator
    MS437 is a potent TSH receptor (TSHR) stimulator with an EC50 value of 13x10-8 M. MS437 shows potent activation of Gsα, Gαq and Gα12 and up-regulation of thyroglobulin (Tg), sodium iodine symporter (NIS) and TSHR gene expressions.
    MS437
  • HY-169054
    NCATS-SM4420
    NCATS-SM4420 (Compound A35) is an orally active thyroid-stimulating hormone receptor (TSHR) ligand that inhibits the proliferation of MDA-T32 and MDA-T85 cells in vitro (IC50 values of 0.71 μM and 0.38 μM, respectively) and suppresses metastasis of MDA-T85F1 in mice. NCATS-SM4420 holds promise for research in the field of thyroid cancer.
    NCATS-SM4420
  • HY-100271
    Org41841
    		Agonist 99.77%
    Org41841 is a partial agonist of both luteinizing hormone/chorionic gonadotropin receptor (LHCGR) and thyroid-stimulating hormone receptor (TSHR) with EC50s of 0.2 and 7.7 μM, respectively.
    Org41841
  • HY-18286
    NCGC00229600
    		Antagonist 99.67%
    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.
    NCGC00229600
  • HY-114918
    MS438
    		Agonist 99.85%
    MS438 is a potent thyrotropin receptor (TSHR) agonist with an EC50 of 53 nM. MS438 binds to the serpentine portion of the TSHR. MS438 induces T4 secretion in mice.
    MS438
  • HY-122974
    VA-K-14 hydrochloride
    		Antagonist 98.20%
    VA-K-14 hydrochloride is a specific thyroid-stimulating hormone receptor (TSHR) antagonist (IC50= 12.3 μM).
    VA-K-14 hydrochloride
  • HY-124867
    D3-βArr
    		Modulator 99.49%
    D3-βArr is a positive allosteric modulator for thyrotropin receptor (TSHR), which initiates translocation of β-Arr 1 by direct TSHR activation and potentiates TSH-mediated preosteoblast differentiation in vitro.
    D3-βArr
  • HY-129995
    TSHR antagonist S37b
    		Inhibitor 99.06%
    TSHR antagonist S37b is the less effective enantiomer of TSHR antagonist S37a (HY-129995A). TSHR antagonist S37b shows only a minor effect for thyrotropin receptor (TSHR) inhibition. TSHR antagonist S37b can be used for the research of thyroid function.
    TSHR antagonist S37b
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