| Description | ML-180 (SR1848) is a potent orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) inverse agonist (IC50 of 3.7 μM) . |
| In vitro | ML-180(0.5-5 μM;24小时)在肝细胞中显著抑制cyclin-D1和cyclin-E1的表达,然而对SK-OV-3细胞的抑制作用不明显[2]。ML-180(5 μM;24小时)迅速降低LRH-1的表达,并有效抑制内源性LRH-1信号传导[2]。 |
| In vivo | ML-180在肾上腺和胰腺组织中显著降低LRH-1和SHP mRNA的表达[2]。 |
| Target activity | LRH1:3.7 µM (IC50) |
| Synonyms | SR1848 |
| molecular weight | 388.89 |
| Molecular formula | C20H25ClN4O2 |
| CAS | 863588-32-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 11 mg/mL (28.28 mM), Sonication is recommended. |
| References | 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. |