ML224

1338824-21-7

C31H31N3O5

DMSO : 100 mg/mL (190.26 mM; Need ultrasonic); H2O : < 0.1 mg/mL (insoluble)

GPCR/G Protein

ML224(NCGC00242364; ANTAG3) is a selective TSHR inverse agonist; inhibits TSH-stimulated cAMP production with an IC50 = 2.3 uM. IC50 value: 2.3 uM [1] Target: TSHR agonist in vitro: ANTAG3 was selective for TSHR inhibition; half-maximal inhibitory doses were 2.1 uM for TSHR and greater than 30 uM 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].