• 产品描述： ML-180 (SR1848) is a potent orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) inverse agonist with an IC50 of 3.7 µM. ML-180 is inactive for steroidogenic factor-1 (SF-1; NR5A1; IC50>10 µM). ML-180 has the potential for LRH-1-dependent cancers

• 靶点： IC50: 3.7 µM (LRH-1)

• 体外研究：
  ML-180 (SR1848; 0.01-100 µM; 48 hours) shows diminished capacity to proliferate at concentrations above 1 μM, and the EC50 being roughly 2.8 μM in Huh-7 cells. ML-180 inhibits cell proliferation in an LRH-1-dependent manner. ML-180 (0.5-5 µM; 24 hours) shows a significant inhibition of cyclin-D1 and cyclin-E1 expression in hepatic cells, but has little effect on repression in SK-OV-3 cells. ML-180 (5 µM; 24 hours) leads to a rapid decrease of LRH-1 expression and efficiently represses endogenous LRH-1 signaling. ML-180 (0.5-5 µM; 24 hours) inhibits LRH-1 mRNA expression in a dose-dependent manner. ML-180 (5 μM; 2 hours) rapidly and significantly decreases the mRNA levels of LRH-1 receptor and its downstream targets (CYP19, GATA3, and GATA4) in Huh-7 and HepG2 cells. Cell Proliferation Assay Cell Line: Huh-7 cells Concentration: 0.01, 0.1, 1, 10, 100 µM Incubation Time: 48 hours Result: Showed diminished capacity to proliferate at concentrations above 1 μM. Cell Cycle Analysis Cell Line: Huh-7 cells Concentration: 0.5, 1, 5 µM Incubation Time: 24 hours Result: Showed a significant inhibition of cyclin-D1 and cyclin-E1 expression in hepatic cells. Western Blot Analysis Cell Line: Huh-7 cells Concentration: 5 µM Incubation Time: 24 hours Result: Significantly reduced the LRH-1 protein levels. RT-PCR Cell Line: Huh-7 cells Concentration: 0.5, 1, 5 µM Incubation Time: 24 hours Result: Inhibited LRH-1 mRNA expression in a dose-dependent manner.

• 体内研究：
  ML-180 (SR1848; 30 mg/kg; i.p.; daily; for 10 days) has a statistically significant decrease of both LRH-1 and SHP mRNA in adrenal glands and pancreatic tissue. Animal Model: 8-week-old C57Bl/6J mice Dosage: 30 mg/kg Administration: IP; daily; for 10 days Result: Had a statistically significant decrease of both LRH-1 and SHP mRNA in adrenal glands and pancreatic tissue.

• 参考文献：
  1. Busby S, et al. Discovery of Inverse Agonists for the Liver Receptor Homologue-1 (LRH1; NR5A2). 2. Corzo CA, et al. Antiproliferation activity of a small molecule repressor of liver receptor homolog 1. Mol Pharmacol. 2015 Feb;87(2):296-304.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20°C

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.571 ml	12.857 ml	25.714 ml
  5 mM	0.514 ml	2.571 ml	5.143 ml
  10 mM	0.257 ml	1.286 ml	2.571 ml
  50 mM	0.051 ml	0.257 ml	0.514 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 *