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ML-180 (Synonyms: SR1848)

Cat. No.: HY-115613 Purity: 99.85%
Handling Instructions

ML-180 (SR1848) is a potent orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) inverse agonist with an IC50 of 3.7 µM. ML-180 is inactive for steroidogenic factor-1 (SF-1; NR5A1; IC50>10 µM). ML-180 has the potential for LRH-1-dependent cancers.

For research use only. We do not sell to patients.

ML-180 Chemical Structure

ML-180 Chemical Structure

CAS No. : 863588-32-3

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10 mM * 1 mL in DMSO USD 88 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 130 In-stock
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50 mg USD 420 In-stock
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100 mg USD 680 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

ML-180 (SR1848) is a potent orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) inverse agonist with an IC50 of 3.7 µM. ML-180 is inactive for steroidogenic factor-1 (SF-1; NR5A1; IC50>10 µM). ML-180 has the potential for LRH-1-dependent cancers[1][2].

IC50 & Target

IC50: 3.7 µM (LRH-1)[1]

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[2].
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[2].
ML-180 (5 µM; 24 hours) leads to a rapid decrease of LRH-1 expression and efficiently represses endogenous LRH-1 signaling[2].
ML-180 (0.5-5 µM; 24 hours) inhibits LRH-1 mRNA expression in a dose-dependent manner[2].
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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

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[2]

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[2]

Cell Line: Huh-7 cells
Concentration: 5 µM
Incubation Time: 24 hours
Result: Significantly reduced the LRH-1 protein levels.

RT-PCR[2]

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.
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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 8-week-old C57Bl/6J mice[2]
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.
Molecular Weight

388.89

Formula

C₂₀H₂₅ClN₄O₂

CAS No.

863588-32-3

SMILES

O=C1N(C2CCCCC2)C(C=C(N3CCN(C4=CC=CC(Cl)=C4)CC3)N1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 11.9 mg/mL (30.60 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5714 mL 12.8571 mL 25.7142 mL
5 mM 0.5143 mL 2.5714 mL 5.1428 mL
10 mM 0.2571 mL 1.2857 mL 2.5714 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.19 mg/mL (3.06 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.19 mg/mL (3.06 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.85%

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Keywords:

ML-180SR1848ML180ML 180SR 1848SR-1848OthersOrphannuclearreceptorliverhomologLRH-1NR5A2steroidogenicfactor-1SF-1NR5A1cancersInhibitorinhibitorinhibit

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ML-180
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