ML-180

SKU: orb1219596

Description

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.

Key Properties

• CAS Number: 863588-32-3
• MW: 388.89
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₅ClN₄O₂
• SMILES: Clc1cccc(c1)N1CCN(CC1)c1cc(=O)n(C2CCCCC2)c(=O)[nH]1
• Target: orphan nuclear receptor NR5A2
• Solubility: DMSO:11 mg/mL (28.28 mM; Need ultrasonic)

Bioactivity

• 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. 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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SR1848

Quick Database Links

Gene Symbol

orphan nuclear receptor NR5A2