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• 产品描述： 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.

• 靶点： TSHR:2.1 μM (IC50);LHR:＞30 μM (IC50);FSHR:＞30 μM (IC50);TSHReceptor

• 体外研究：
  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. Cell Viability Assay Cell Line: Human embryonic kidney 293 cells (stably expressing TSHRs, LHRs, or FSHRs) Concentration: 0.001-100 µM Incubation Time: 20 min Result: Showed the IC50 for stimulation by bovine TSH (1.8 nM) was 2.1 µM.Showed inhibition of LH and FSH stimulation was less than 15% for LH (1 nM) and less than 30% for FSH (1 nM) at 30 µM.

• 体内研究：
  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. Animal Model: Female BALB/c mice (8 to 13-week-old; ~18.7 g). Dosage: 2 mg/mice Administration: Intraperitoneal injection via osmotic pump; single daily for 3 days Result: Lowered the levels of FT4 by 44%, and the levels of TPO and NIS mRNAs by 75% and 83%, respectively.

• 参考文献：
  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.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.903 ml	9.513 ml	19.026 ml
  5 mM	0.381 ml	1.903 ml	3.805 ml
  10 mM	0.19 ml	0.951 ml	1.903 ml
  50 mM	0.038 ml	0.19 ml	0.381 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *