CAS:1186649-91-1N-(4-((5-(3-Benzyl-5-hydroxy-4-oxo-1,2,3,4-tetrahydroquinazolin-2-yl)-2-methoxybenzyl)oxy)phenyl)acetamide

Synonyms: ML-109

ML-109 is a potent and full thyroid stimulating hormone receptor (TSHR) agonist with EC50 of 40 nM.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

技术信息

CAS号

1186649-91-1

储存条件

分子式

C31H29N3O5

运输

蓝冰

分子量

523.58

别名

ML-109

溶解度

DMSO	80.0 mg/mL (152.8 mM) warming

动物实验配方

生物活性

描述The thyrotropin (thyroid-stimulating hormone, TSH) receptor (TSHR) is the third member of the glycoprotein hormone receptor subfamily. TSH is secreted into the circulation in response to TSH-releasing hormone stimulation and in turn stimulates the function of the thyroid follicular cells. ML-109 is a full agonist at TSHR with an EC₅₀ of 40 nM. After 24 h, treatment of thyrocytes with ML-109 increased TG, TPO, NIS, and DIO2 mRNAs. It increased TG mRNA as effectively as TSH. Both TSH and ML-109 increased DIO2 protein activity. ML-109 (0.5 mg) increased serum T4 to a level that was not statistically different from the increase with TSH in mice after i.p. administration. Moreover, ML-109 elevated serum T4 and, perhaps more importantly if it were to be used as a lead drug, stimulated radioiodide uptake by the mouse thyroid gland in mice by esophageal gavage^[1].
作用机制ML-109 binds to the serpentine region of TSHR^[1].