ML-180(Synonyms: SR1848)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ML-180 (Synonyms: SR1848) 纯度: 99.85%

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 µM。ML-180 不抑制类固醇生成因子 1 (SF-1; NR5A1; IC50>10 µM)。 ML-180 具有抗依赖 LRH-1 癌症的潜力。

ML-180(Synonyms: SR1848)

ML-180 Chemical Structure

CAS No. : 863588-32-3

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10 mM * 1 mL in DMSO ￥880 In-stock
5 mg ￥800 In-stock
10 mg ￥1300 In-stock
50 mg ￥4200 In-stock
100 mg ￥6800 In-stock
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ML-180 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Transcription Factor Targeted Library

生物活性

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]
体外研究
(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].

上海金畔生物科技有限公司 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.

体内研究
(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].

上海金畔生物科技有限公司 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.

分子量

388.89

Formula

C20H25ClN4O2
CAS 号

863588-32-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, stored under nitrogen

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

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

配制储备液
浓度 溶剂体积 质量 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

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

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

    此方案可获得 ≥ 1.19 mg/mL (3.06 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 11.9 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

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

    此方案可获得 ≥ 1.19 mg/mL (3.06 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 11.9 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [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.

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