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GPCR/G Protein

Melanin-concentrating Hormone Receptor (MCHR)

(10)

Melanocortin Receptor

Neuropeptide Y Receptor

Prostaglandin Receptor

(161)

Protease-activated Receptor

TSH Receptor

The thyrotropin receptor (or TSH receptor) is a receptor (and associated protein) that responds to thyroid-stimulating hormone (also known as "thyrotropin") and stimulates the production of thyroxine (T4) and triiodothyronine (T3). The TSH receptor is a member of the G protein-coupled receptor superfamily of integral membrane proteins and is coupled to the Gs protein.

Filter HomeSignaling PathwaysGPCR/G ProteinTSH Receptor

ML224

T161061338824-21-7

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

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ML-109

T120731186649-91-1

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

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Cited

TSHR antagonist S37

T132161217616-61-9

TSHR antagonist S37 is a selective and competitive antagonist of the thyrotropin receptor (TSHR).

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VA-K-14 hydrochloride

T290871171341-19-7In house

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.

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D3-βArr

T5383662164-09-2

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.

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NCGC00229600

T121921338824-20-6

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.

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Teprotumumab

T767271036734-93-6

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.

$163

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Org41841

T16403301847-37-0

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.

$199

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