ML224 (NCGC00242364) is a selective TSHR antagonist with an IC50 value of 2.1 μM. ML224 can be used in the study of Graves' disease and other thyroid disorders.
ChEBI: N-[4-[[5-[3-(2-furanylmethyl)-4-oxo-1,2-dihydroquinazolin-2-yl]-2-methoxyphenyl]methoxy]-3,5-dimethylphenyl]acetamide is a member of quinazolines.
ANTAG3 (2 mg/mice; i.p. via osmotic pump; single daily for 3 days) lowers serum FT4 levels and thyroidal mRNAs for TPO and NIS in mice continuously stimulated by TRH[1].
| Animal Model: | Female BALB/c mice (8 to 13-week-old; ~18.7 g)[1]. |
| Dosage: | 2 mg/mice |
| Administration: | Intraperitoneal injection via osmotic pump; single daily for 3 days |
| Result: | Lowered the levels of FT4 by 44%, and the levels of TPO and NIS mRNAs by 75% and 83%, respectively. |
TSHR: 2.1 μM (IC50); LHR: ＞30 μM (IC50); FSHR: ＞30 μM (IC50)
[1] Neumann S, et al. A selective TSH receptor antagonist inhibits stimulation of thyroid function in female mice. Endocrinology. 2014 Jan;155(1):310-4. DOI:
10.1210/en.2013-1835
