ML-180 SR1848|cas:863588-32-3|西域试剂

ML-180 SR1848,99.82%

产品编号：Bellancom-115613| CAS NO：863588-32-3| 分子式：C₂₀H₂₅ClN₄O₂| 分子量：388.89

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货号	价格	库存与货期
Bellancom-115613	￥800.00	杭州北京（现货）
Bellancom-115613	￥1300.00	杭州北京（现货）
Bellancom-115613	￥4200.00	杭州北京（现货）
Bellancom-115613	￥6800.00	杭州北京（现货）

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ML-180 SR1848

产品介绍

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。

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.

体外研究

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.

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

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.

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.

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

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.

体内研究

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.

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

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.

体内研究

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.

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

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.

性状

Solid

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。