ML224

Research use only, not for human use.

ML224 (NCGC00242364) is a TSHR antagonist for the treatment of Graves' orbital disease and Graves' hyperthyroidism.

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.

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.

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.

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Others

Other Targets

TSH Receptor

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1338824-21-7

525.59

C31H31N3O5

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (190.26 mM; Ultrasonic )

COc1ccc(cc1COc1c(C)cc(NC(C)=O)cc1C)C1Nc2ccccc2C(=O)N1Cc1ccco1

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(-20℃)

With Ice Pack

≥ 2 years