ML224

ML224 (NCGC00242364) is a selective TSHR antagonist with an IC 50 value of 2.1 µM. ML224 can be used in the study of Graves' disease and other thyroid disorders. In Vitro ML224 (0.001-100 μM; 20 min) exhibits half-maximal inhibitory doses of 2.1 μM for TSHR and greater than 30 μM for LH and FSH receptors in human embryonic kidney 293 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Human embryonic kidney 293 cells (stably expressing TSHRs, LHRs, or FSHRs) Concentration: 0.001-100 µM Incubation Time: 20 min Result: Showed the IC 50 for stimulation by bovine TSH (1.8 nM) was 2.1 µM. Showed inhibition of LH and FSH stimulation was less than 15% for LH (1 nM) and less than 30% for FSH (1 nM) at 30 µM. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female BALB/c mice (8 to 13-week-old; ~18.7 g) . 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. IC50& Target:TSHR 2.1 μM (IC 50 ) LHR ＞30 μM (IC 50 ) FSHR ＞30 μM (IC 50 )

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