1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEML-180Cat. No.: HY-115613CAS No.: 863588-32-3Synonyms: SR1848分式: CHClNO分量: 388.89作靶點: Others作通路: Others儲存式: Please store the product under the recommended conditions inthe COA.BIOLOGICAL ACTIVITY物活性 ML-180 (SR1848)種有效的孤核受體肝受體同物

2、1 (LRH-1; NR5A2) 反向激動劑，IC50 為 3.7 M。ML-180 不抑制類醇成因 1 (SF-1; NR5A1; IC5010 M)。 ML-180 具有抗依賴 LRH-1 癌癥的潛。IC50 & Target IC50: 3.7 M (LRH-1) 1體外研究ML-180 (SR1848; 0.01-100 M; 48 hours) shows diminished capacity to proliferate at concentrations above 1M, and the EC50 being roughly 2.8 M in Huh-7 cells. ML-

3、180 inhibits cell proliferation in an LRH-1-dependent manner 2.ML-180 (0.5-5 M; 24 hours) shows a significant inhibition of cyclin-D1 and cyclin-E1 expression in hepaticcells, but has little effect on repression in SK-OV-3 cells 2.ML-180 (5 M; 24 hours) leads to a rapid decrease of LRH-1 expression

4、and efficiently repressesendogenous LRH-1 signaling 2.ML-180 (0.5-5 M; 24 hours) inhibits LRH-1 mRNA expression in a dose-dependent manner 2.ML-180 (5 M; 2 hours) rapidly and significantly decreases the mRNA levels of LRH-1 receptor and itsdownstream targets (CYP19, GATA3, and GATA4) in Huh-7 and He

5、pG2 cells 2.Cell Proliferation Assay 2Cell Line: Huh-7 cellsConcentration: 0.01, 0.1, 1, 10, 100 M1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEIncubation Time: 48 hoursResult: Showed diminished capacity to proliferate at concentrations above 1 M.Cell Cycle Analysis 2Cell Line: Huh-7 cellsConcent

6、ration: 0.5, 1, 5 MIncubation Time: 24 hoursResult: Showed a significant inhibition of cyclin-D1 and cyclin-E1 expression in hepatic cells.Western Blot Analysis 2Cell Line: Huh-7 cellsConcentration: 5 MIncubation Time: 24 hoursResult: Significantly reduced the LRH-1 protein levels.RT-PCR 2Cell Line:

7、 Huh-7 cellsConcentration: 0.5, 1, 5 MIncubation Time: 24 hoursResult: Inhibited LRH-1 mRNA expression in a dose-dependent manner.體內研究 ML-180 (SR1848; 30 mg/kg; i.p.; daily; for 10 days) has a statistically significant decrease of both LRH-1 andSHP mRNA in adrenal glands and pancreatic tissue 2.Anim

8、al Model: 8-week-old C57Bl/6J mice 2Dosage: 30 mg/kgAdministration: IP; daily; for 10 daysResult: Had a statistically significant decrease of both LRH-1 and SHP mRNA in adrenal glandsand pancreatic tissue.REFERENCES2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. 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.McePdfHeightCaution: Product has not been fully validated for medical ap