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-107916
    Thyrotropin
    Thyrotropin (TSH, Pretiron) is a thyroid-stimulating hormone produced by thyrotrope cells in the anterior pituitary gland. Thyrotropin regulates the endocrine function of the thyroid. Thyrotropin induces transcriptional regulation of TH-gatekeeper genes in tanycytes through the Tshr/Gαq/PKC pathway. Thyrotropin prevents Apoptosis. Thyrotropin has an association of low levels with increased bone remodeling, reduced bone mass and a high fracture risk in mice. Thyrotropin is promising for research of skeletal remodeling, hyperthyroidism.
    Thyrotropin
  • HY-114116
    ML-109
    		Agonist 99.02%
    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-114994
    MS437
    		Activator ≥98.0%
    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-153213
    Org 274179-0
    		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).
    Org 274179-0
  • 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-P990534
    Anti-TSHR Antibody (K1-70)
    		98.57%
    Anti-TSHR Antibody (K1-70) is a CHO-expressed human antibody that targets TSHR. Anti-TSHR Antibody (K1-70) has a huIgG1 heavy chain and a huλ light chain, with a predicted molecular weight (MW) of 143.54 kDa. For the isotype control of Anti-TSHR Antibody (K1-70), you can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-TSHR Antibody (K1-70)
  • HY-158100
    SYD5115
    		Antagonist 99.69%
    SYD5115 is an orally available TSH-R antagonist.
    SYD5115
  • 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-122974
    VA-K-14 hydrochloride
    		Antagonist 98.96%
    VA-K-14 hydrochloride is a specific thyroid-stimulating hormone receptor (TSHR) antagonist (IC50= 12.3 μM).
    VA-K-14 hydrochloride
  • 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-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-107380A
    PGlu-3-methyl-His-Pro-NH2 TFA
    		99.69%
    PGlu-3-methyl-His-Pro-NH2 TFA (A-42872 TFA), the modified thyrotropin-releasing hormone (TRH) peptide, enhances binding to pituitary TRH receptors and increases stimulation of thyroid-stimulating hormone (TSH) release from the pituitary. The in vitro permeability of PGlu-3-methyl-His-Pro-NH2 TFA through rat skin is increased in the presence of enhancers Ethanol and Cineole.
    PGlu-3-methyl-His-Pro-NH2 TFA
  • 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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