ML-180

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ML-180 是一种有效的孤儿核受体肝受体同源物 1 (LRH-1; NR5A2) 反向激动剂（IC50 为 3.7 μM）。ML-180（0.5-5 μM；24 小时）显示出对 cyclin-D1 和 cyclin-D1 的显着抑制作用。 cyclin-E1 在肝细胞中的表达，但对 SK-OV-3 细胞中的抑制影响不大[2]。 ML-180（5 μM；24 小时）导致 LRH-1 表达快速降低，并有效抑制内源性 LRH-1 信号传导。

ML-180 is a potent orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) inverse agonist (IC50 of 3.7 μM) .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 has a statistically significant decrease of both LRH-1 and SHP mRNA in adrenal glands and pancreatic tissue.

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-PCRCell 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.

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.

SR1848

Others

Other Targets

orphan nuclear receptor NR5A2

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863588-32-3

388.89

C20H25ClN4O2

>98% (HPLC)

DMSO:11 mg/mL (28.28 mM; Need ultrasonic)

Clc1cccc(c1)N1CCN(CC1)c1cc(=O)n(C2CCCCC2)c(=O)[nH]1

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(-20℃)

With Ice Pack

≥ 2 years