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CAS No.: 1186649-91-1

ML-109 Catalog No. CSN25322

Synonyms: CID-25246343

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

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生物活性

实验方案

技术信息

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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9099 mL
- 9.5497 mL
- 19.0993 mL
- 5 mM
- 0.3820 mL
- 1.9099 mL
- 3.8199 mL
- 10 mM
- 0.1910 mL
- 0.9550 mL
- 1.9099 mL

技术信息

CAS号

1186649-91-1

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C31H29N3O5

运输

蓝冰

分子量

523.58

别名

CID-25246343

溶解度

DMSO	80.0 mg/mL (152.8 mM) warming

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ML-109 Catalog No. CSN25322

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