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ML-180

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Chemical Structure| 863588-32-3 同义名 : SR1848;CID-3238389
CAS号 : 863588-32-3
货号 : A1210813
分子式 : C20H25ClN4O2
纯度 : 99%+
分子量 : 388.891
MDL号 : MFCD05894342
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 12 mg/mL(30.86 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.86mL

2.57mL

1.29mL

25.71mL

5.14mL

2.57mL
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