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.
性状
Solid
IC50 & Target[1][2]
TSHR
2.1 μM (IC50)
LHR
>30 μM (IC50)
FSHR
>30 μM (IC50)
体外研究(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.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay
Cell Line:
Human embryonic kidney 293 cells (stably expressing TSHRs, LHRs, or FSHRs)
Concentration:
0.001-100 μM
Incubation Time:
20 min
Result:
Showed the IC50 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.
体内研究(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.
Medlife 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.