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CAS No.: 863588-32-3

ML-180 Catalog No. CSN27223

Synonyms: CID-3238389;SR1848

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 .

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技术信息

生物活性

描述LRH1 (liver receptor homologue-1; NR5A2) belongs to the four-member NR5A, or Ftz-F1, subfamily V of nuclear receptors. LRH1 regulates expression of Cyp19 (aromatase) and promotes motility and invasiveness in ER-positive breast cancer cells, suggesting LRH1 as a target for inverse agonists for the treatment of ER-positive breast cancers. ML-180 is an effective antagonist of LRH1 with an IC₅₀ value of 3.7 μM^[3]. In granulosa cells from superstimulated immature CON mice, ML-180 (3 µM; 6 hr) caused a demonstrable reduction in transcripts for Ccnd1, Ccnd2, Ccne1, and E2f1. At 24 hours of treatment, proliferation was suppressed by one-half^[4].
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.
[3] Busby S, et al. Discovery of Inverse Agonists for the Liver Receptor Homologue-1 (LRH1; NR5A2). 2010 Oct 12
[4] Meinsohn MC, et al. The Orphan Nuclear Receptor Liver Homolog Receptor-1 (Nr5a2) Regulates Ovarian Granulosa Cell Proliferation. J Endocr Soc. 2017 Dec 1;2(1):24-41

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5714 mL
- 12.8571 mL
- 25.7141 mL
- 5 mM
- 0.5143 mL
- 2.5714 mL
- 5.1428 mL
- 10 mM
- 0.2571 mL
- 1.2857 mL
- 2.5714 mL

技术信息

CAS号	863588-32-3	储存条件	粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C20H25ClN4O2	运输	蓝冰
分子量	388.89	别名	CID-3238389;SR1848

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