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ML-180

CAS No. : 863588-32-3

MCE 站：ML-180

产品活性：ML-180 (SR1848) 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 ?M。ML-180 不抑制类固醇生成因子 1 (SF-1; NR5A1; IC₅₀>10 ?M)。 ML-180 具有抗依赖 LRH-1 癌症的潜力。

研究领域：Others

作用靶点：Others

In Vitro: ML-180 (SR1848; 0.01-100 ?M; 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 ?M; 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 ?M; 24 hours) leads to a rapid decrease of LRH-1 expression and efficiently represses endogenous LRH-1 signaling.
ML-180 (0.5-5 ?M; 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.

In Vivo: 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.

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