TSH Receptor

Total: 11
Updated: 2019-06-28 15:55:20
The thyrotropin receptor (TSHR), one of the primary antigens in autoimmune thyroid disease, is a target of both antigen-specific T cells and antibodies in patients with this condition. Autoantibodies to the TSHR (TSHR-Ab) act as thyroid stimulating factor (TSH) agonists in autoimmune hyperthyroidism (Robert Graves disease) but as TSH antagonists in autoimmune hypothyroidism (Hashimoto thyroiditis). The TSHR antigen is primarily expressed in the epithelial cells of the thyroid follicles, but TSHR mRNA and protein have been reported in a variety of cell types, some of which show evidence of receptor activity. TSH receptor (TSHR) plays an important role in the pathogenesis of thyroid disease, a TSHR antagonist could be a novel treatment. TSH, acting through the TSH receptor, is the major stimulator of thyroid cell growth, differentiation and function.

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Neuronal Signaling >
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NF-κB >
NF-κB IKK Keap1-Nrf2 MALT1
PI3K/Akt/mTOR >
Akt AMPK ATM/ATR DNA-PK GSK-3 MELK mTOR PDK-1 PI3K PI4K PIKfyve PTEN
PROTAC >
PROTAC E3 Ligase Ligand-Linker Conjugate Ligand for E3 Ligase PROTAC Linker PROTAC-linker Conjugate for PAC
Protein Tyrosine Kinase/RTK >
Ack1 ALK Bcr-Abl BMX Kinase Btk c-Fms c-Kit c-Met/HGFR Discoidin Domain Receptor DYRK EGFR Ephrin Receptor FAK FGFR FLT3 IGF-1R Insulin Receptor IRAK Itk PDGFR PKA Pyk2 ROS Src Syk TAM Receptor Trk Receptor VEGFR
Stem Cell/Wnt >
Casein Kinase ERK Gli GSK-3 Hedgehog Hippo (MST) JAK Notch Oct3/4 PKA Porcupine ROCK sFRP-1 Smo STAT TGF-beta/Smad Wnt YAP β-catenin γ-secretase
TGF-beta/Smad >
TGF-beta/Smad PKC ROCK TGF-β Receptor
Vitamin D Related >
VD/VDR
Others >
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Org41841

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.

  • CAS Number: 301847-37-0
  • MF: C19H22N4O2S2
  • MW: 402.534
  • Catalog: TSH Receptor
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
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  • Flash Point: N/A
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MS438

MS438 is a potent agonist of the TSH receptor (TSHR).

  • CAS Number: 512840-45-8
  • MF: C20H17F3N2O3
  • MW: 390.36
  • Catalog: TSH Receptor
  • Density: N/A
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TSHR antagonist S37b

TSHR antagonist S37b is an enantiomer of TSHR antagonist S37a (HY-129995A), shows only a minor effect for TSHR inhibition. TSHR antagonist S37b can be used for the research of thyroid function[1].

  • CAS Number: 2143452-22-4
  • MF: C25H20N2O3S2
  • MW: 460.57
  • Catalog: TSH Receptor
  • Density: N/A
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NCGC00379308

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[1].

  • CAS Number: 662164-09-2
  • MF: C20H23N5
  • MW: 333.43
  • Catalog: TSH Receptor
  • Density: N/A
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TSHR antagonist S37a

TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy[1].

  • CAS Number: 2143452-20-2
  • MF: C25H20N2O3S2
  • MW: 460.57
  • Catalog: TSH Receptor
  • Density: N/A
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VA-K-14 hydrochloride

VA-K-14 hydrochloride is a specific thyroid-stimulating hormone receptor (TSHR) antagonist (IC50= 12.3 μM)[1].

  • CAS Number: 1171341-19-7
  • MF: C18H16ClN3S
  • MW: 305.397
  • Catalog: TSH Receptor
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 510.1±52.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 262.3±30.7 °C
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Teprotumumab

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[1].

  • Density: N/A
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ML-109

ML-109 is a potent and full thyroid stimulating hormone receptor (TSHR) agonist, with an EC50 of 40 nM.

  • CAS Number: 1186649-91-1
  • MF: C31H29N3O5
  • MW: 523.58
  • Catalog: TSH Receptor
  • Density: N/A
  • Boiling Point: N/A
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TSHR antagonist S37

TSHR antagonist S37 is a selective and competitive thyrotropin receptor (TSHR) antagonist. TSHR antagonist S37 is the racemate of TSHR antagonist S37a[1].

  • CAS Number: 1217616-61-9
  • MF: C25H20N2O3S2
  • MW: 460.57
  • Catalog: TSH Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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NCGC00229600

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[1].

  • CAS Number: 1338824-20-6
  • MF: C30H29N3O3
  • MW: 479.57
  • Catalog: TSH Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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ML-224

ML224(NCGC00242364; ANTAG3) is a selective TSHR inverse agonist; inhibits TSH-stimulated cAMP production with an IC50 = 2.3 μM.IC50 value: 2.3 uM [1]Target: TSHR agonistin vitro: ANTAG3 was selective for TSHR inhibition; half-maximal inhibitory doses were 2.1 μM for TSHR and greater than 30 μM for LH and FSH receptors [2]. in vivo: In mice treated with TRH, ANTAG3 lowered serum free T4 by 44% and lowered mRNAs for sodium-iodide cotransporter and thyroperoxidase by 75% and 83%, respectively. In mice given M22, ANTAG3 lowered serum free T4 by 38% and lowered mRNAs for sodium-iodide cotransporter and thyroperoxidase by 73% and 40%, respectively [2].

  • CAS Number: 1338824-21-7
  • MF: C31H31N3O5
  • MW: 525.595
  • Catalog: TSH Receptor
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 752.3±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 408.8±32.9 °C
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