ML224 is a selective TSHR inverse agonist. ML224 also inhibits TSH-stimulated cAMP production (IC50 = 2.3 μM).

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].

ANTAG3 lowered serum-free T4 by 44% and lowered mRNAs for sodium-iodide cotransporter and thyroperoxidase by 75% and 83%, respectively, in mice treated with TRH. ANTAG3 lowered serum-free T4 by 38% and lowered mRNAs for sodium-iodide cotransporter and thyroperoxidase by 73% and 40%, respectively, in mice given M22 [2].

1338824-21-7

C31H31N3O5

525.59

NCGC00242364;ANTAG3

DMSO:100 mg/mL (190.26 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years