ML-109

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Chemical Structure| 1186649-91-1 同义名 : -
CAS号 : 1186649-91-1
货号 : A1176977
分子式 : C31H29N3O5
纯度 : 99%+
分子量 : 523.58
MDL号 : MFCD31746908
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

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
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].
实验方案
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
参考文献

[1]Neumann S, Huang W, Titus S, et al. Small-molecule agonists for the thyrotropin receptor stimulate thyroid function in human thyrocytes and mice. Proc Natl Acad Sci U S A. 2009;106(30):12471-12476