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]. |
计算器 | ||||
存储液制备 | ![]() | 1mg | 5mg | 10mg |
1 mM 5 mM 10 mM | 1.91mL 0.38mL 0.19mL | 9.55mL 1.91mL 0.95mL | 19.10mL 3.82mL 1.91mL |
CAS号 | 1186649-91-1 |
分子式 | C31H29N3O5 |
分子量 | 523.579 |
别名 | |
运输 | 蓝冰 |
存储条件 | In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,2-8°C |
溶解方案 | DMSO: 85 mg/mL(162.34 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |