| Bioactivity | 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. | ||||||||||||
| Invitro | 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[1]. Cell Viability Assay[1] Cell Line: | ||||||||||||
| 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[1]. Animal Model: | ||||||||||||
| Name | ML224 | ||||||||||||
| CAS | 1338824-21-7 | ||||||||||||
| Formula | C31H31N3O5 | ||||||||||||
| Molar Mass | 525.59 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |