NCGC00229600 is a small molecule, allosteric inverse agonist of TSH receptor (TSHR), inhibits basal cAMP production by TSHRs by 53% at 30 uM.
NCGC00229600 shows no effect on [125I]TSH binding to HEKTSHR cells, no effect on the binding of two monoclonal anti-TSHR antibodies, 2C11 and 4C1.
NCGC00229600 is an antagonist of basal and hTSH stimulation of hTSHR in human cells.
NCGC00229600 inhibits TSHR-mediated basal and GD sera up-regulation of thyroperoxidase mRNA levels by 65 ± 2.0% in primary cultures of human thyrocytes.
