TSH Receptor
Thyrotropin receptor; Thyroid-stimulating hormone Receptor
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.
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TSH Receptor Related Products (24)
Related Products (24)
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Recombinant Proteins (2)
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Antibodies (2)
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Anti-TSHR Antibody (M22)
0 ImagesCat. No.: HY-P991202Purity: 98.56%Anti-TSHR Antibody (M22) is a selective agonist targeting TSHR (thyroid-stimulating hormone receptor), acting through competitive binding to the extracellular domain of TSHR. Anti-TSHR Antibody (M22) can mimic the biological effects of thyroid-stimulating hormone (TSH), activating downstream cAMP-PKA and other signaling pathways. Anti-TSHR Antibody (M22) can stimulate the proliferation of thyroid follicular epithelial cells and human umbilical vein endothelial cells (HUVECs), promote angiogenesis and tube formation, cell migration, and also upregulate the expression of angiogenesis-related proteins such as PROX1. Anti-TSHR Antibody (M22) can be used in research areas such as the mechanisms of goiter formation in Graves' disease (GD), angiogenesis regulation, and TSHR antagonist screening.
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Teprotumumab
0 ImagesTeprotumumab 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.
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Anti-TSHR Antibody (K1-70)
0 ImagesCat. No.: HY-P990534Purity: 98.57%Synonyms: K1-70Anti-TSHR Antibody (K1-70) is an anti-TSHR monoclonal antibody. Anti-TSHR Antibody (K1-70) incorporates a single-chain variable fragment into a chimeric antigen receptor to redirect T cells to TSHR-expressing cells. Anti-TSHR Antibody (K1-70) shows antitumor activity with no apparent toxicity. Anti-TSHR Antibody (K1-70) can be used for the research of differentiated thyroid cancer (DTC).
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Thyrotropin
0 ImagesThyrotropin (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.
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ML-109
0 ImagesML-109 is a potent and full thyroid stimulating hormone receptor (TSHR) agonist, with an EC50 of 40 nM.
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2"-O-Galloylhyperin
0 Images2''-O-Galloylhyperin is an active natural compound with anti‑inflammatory, antioxidant, anti‑adipogenic, antifibrotic, and cytostatic activities. 2''-O-Galloylhyperin upregulates SIRT1/Nrf2 signaling, inhibits NF-κB and MAPK (ERK1/2, p38, JNK) phosphorylation, suppresses TSHR activation, reduces ROS accumulation, and enhances SOD and GSH-Px activities. 2''-O-Galloylhyperin protects against LPS-induced tissue injury, enhances survival, and inhibits adipogenesis and fibrosis. 2"-O-Galloylhyperin can be used for the research of sepsis, acute lung injury, and thyroid eye disease.
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MS438
0 ImagesMS438 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.
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Org 274179-0
0 ImagesOrg 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).
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NCGC00229600
0 ImagesNCGC00229600 is an allosteric inverse agonist of thyrotropin receptor (TSHR). NCGC00229600 inhibits both TSH and stimulating antibody activation of TSHRs endogenously expressed in Graves' disease.
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TSHR antagonist S37a
0 ImagesTSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy.
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MS437
0 ImagesMS437 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.
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VA-K-14 hydrochloride
0 ImagesVA-K-14 hydrochloride is a specific thyroid-stimulating hormone receptor (TSHR) antagonist (IC50= 12.3 μM).
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D3-βArr
0 ImagesD3-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.
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Org41841
0 ImagesOrg41841 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.
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Benzylthiouracil
0 ImagesSynonyms: 6-Benzyl-2-thiouracilBenzylthiouracil is an active pharmaceutical ingredient against hyperthyroidism.
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Org 274178-0
0 ImagesCat. No.: HY-153213APurity: 99.40%Org 274178-0 is a selective thyroid-stimulating hormone receptor (TSHR) antagonist with a pIC50 value for TSHR is 5.03. Org 274178-0 inhibits the activation of cAMP signaling pathway and phospholipase C (PLC) signaling pathway mediated by thyroid-stimulating hormone (TSH) and TSH receptor-stimulating immunoglobulins (TSIs). Org 274178-0 is promising for research of Graves’ disease and Graves’ ophthalmopathy.
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PGlu-3-methyl-His-Pro-NH2 TFA
0 ImagesCat. No.: HY-107380APurity: 99.69%Synonyms: A-42872 TFAPGlu-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.
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TSHR antagonist S37b
0 ImagesTSHR 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.
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