TSH Receptor

Thyrotropin receptor; Thyroid-stimulating hormone Receptor

TSH Receptor

Related Products

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.

TSH Receptor Related Products (24)
Recombinant Proteins (2)
Antibodies (2)

By Effects:	Inhibitors (6) Agonists (5) Antagonists (7) Activator (1) Modulator (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-P991202

Anti-TSHR Antibody (M22)	Agonist	99.46%
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.

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.

HY-P990534

Anti-TSHR Antibody (K1-70)	Inhibitor	98.57%
Anti-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).

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.

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.

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.

HY-N0526

2"-O-Galloylhyperin	Inhibitor	99.57%
2''-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.

HY-158100

SYD5115	Antagonist	99.69%
SYD5115 is an orally available TSH-R antagonist.

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.

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.

HY-129995A

TSHR antagonist S37a	Antagonist	98.22%
TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy.

HY-153213

Org 274179-0	Antagonist	98.63%
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).

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).

HY-114994

MS437	Activator	98.0%
MS437 is a potent TSH receptor (TSHR) stimulator with an EC₅₀ value of 13x10^-8M. MS437 shows potent activation of G_sα, G_αq and Gα₁₂ and up-regulation of thyroglobulin (Tg), sodium iodine symporter (NIS) and TSHR gene expressions.

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.

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.

HY-W069177

Benzylthiouracil	Inhibitor	98.97%
Benzylthiouracil is an active pharmaceutical ingredient against hyperthyroidism.

HY-153213A

Org 274178-0	Antagonist	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.

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.

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.

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TSH Receptor

TSH Receptor

TSH Receptor Related Products (24)

Recombinant Proteins (2)

Antibodies (2)

TSH Receptor Related Products (24):