Ro 48-8071 fumarate

目录号: HY-18630A 纯度: 99.42%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Ro 48-8071 fumarate 是氧化鲨烯环化酶 (Oxidosqualene cyclase) 抑制剂，IC₅₀ 约为 6.5 nM。

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Ro 48-8071 fumarate Chemical Structure

CAS No. : 189197-69-1

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥556	In-stock
5 mg	￥444	In-stock
10 mg	￥784	In-stock
25 mg	￥1294	In-stock
50 mg	￥1500	In-stock
100 mg	￥2495	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Ro 48-8071 fumarate:

Ro 48-8071 询价

MCE 顾客使用本产品发表的 11 篇科研文献

: Ro 48-8071 fumarate purchased from MCE. Usage Cited in: Oncotarget. 2017 Feb 28;8(9):14860-14875. [Abstract]; Cell death in TS600 glioma cells. Dead cells are visualized with SYTOX Orange 24 hours after treatment with DMSO (mock), 1 μM epirubicin, 10 μM clotrimazole, 5 μM ketoconazole, or 1 μM Ro 48-8071.

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Ro 48-8071 fumarate is an inhibitor of OSC (Oxidosqualene cyclase) with IC₅₀ of appr 6.5 nM.

IC₅₀ & Target

IC50: appr 6.5 nM (Oxidosqualene cyclase)^[1]

体外研究
(In Vitro)

在 HepG2 细胞中，Ro 48 -8071 降低胆固醇合成剂量依赖性，IC₅₀ 值约为 1.5 nM^[1]。Ro 48 -8071 (10 μM) 显著降低 PC-3 前列腺癌细胞的活力，但不降低正常前列腺细胞的活力。Ro 48 -8071 (10-30 μM) 以剂量依赖的方式诱导 LNCaP 和 C4-2 细胞系的凋亡。在用 Ro 48 -8071 处理 24 小时后，去势抵抗性 PC-3 和 DU145 细胞也表现出显著水平的细胞凋亡。Ro 48 -8071 (10-25 μM) 以剂量依赖的方式降低 AR 蛋白的表达。Ro 48 -8071 (0.1-1 μM) 在激素依赖性 LNCaP 和去势抵抗性 PC-3 细胞中剂量依赖性地增加 ERβ 蛋白表达^[2]。使用经过改造以表达人 ERα 或 ERβ 蛋白的哺乳动物细胞，连同 ER 反应性荧光素酶启动子，Ro 48 -8071 剂量依赖性地抑制 17β-雌二醇 (E2) 诱导的 ERα 反应性荧光素酶活性 (IC₅₀，appr 10 μM)，在对细胞无毒的条件下^[3]。

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

体内研究
(In Vivo)

Ro 48 -8071 在每天 150 μmol/kg 时最大程度地降低约 60% 的 LDL-C，在每天 300 μmol/kg 时不会进一步降低，而 HDL-C 在仓鼠中的所有剂量下均保持不变。Ro 48 -8071 (每天≥00 μMol/kg) 增加仓鼠肝脏中的 MOS 量。Ro 48 -8071 (每天 300 μmol/kg) 显著降低仓鼠的 VLDL 分泌^[1]。Ro 48 -8071 (5 或 20 mg/kg) 显著减少小鼠体内肿瘤的生长，而小鼠体重没有减轻。此外，浓度为 20 mg/kg 的 Ro 48 -8071 在测试的时间范围内完全根除了小鼠中监测的 12 种肿瘤中的两种^[2]。Ro 48 -8071 (20 毫克/天/千克体重) 导致 BALB/c 小鼠整个小肠中胆固醇合成的快速和持续抑制 (>50%)。大肠和胃中的甾醇合成也减少^[4]。

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

分子量

564.44

Formula

C₂₇H₃₁BrFNO₆

CAS 号

189197-69-1

性状

固体

颜色

White to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

细胞实验：

H₂O 中的溶解度 : 100 mg/mL (177.17 mM; 超声助溶)

DMSO 中的溶解度 : ≥ 55 mg/mL (97.44 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7717 mL	8.8583 mL	17.7167 mL
5 mM	0.3543 mL	1.7717 mL	3.5433 mL
10 mM	0.1772 mL	0.8858 mL	1.7717 mL

查看完整储备液配制表

* 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 (sealed storage, away from moisture)。-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。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

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

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.43 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.43 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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。
20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.43 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。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。

方案一

请依序添加每种溶剂： PBS
Solubility: 12.5 mg/mL (22.15 mM); 澄清溶液; 超声助溶 (<60°C)

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

该产品水溶性佳，请具体参考实测水 / PBS / Saline 中的溶解度数据。

您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。

纯度 & 产品资料

纯度: 99.42%

选择批次：

Data Sheet (650 KB) SDS (393 KB)

COA (261 KB) RP-HPLC (247 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Morand OH, et al. Ro 48-8.071, a new 2,3-oxidosqualene:lanosterol cyclase inhibitor lowering plasma cholesterol in hamsters, squirrel monkeys, and minipigs: comparison to simvastatin. J Lipid Res. 1997 Feb;38(2):373-90. [Content Brief]

[2]. Liang Y, et al. Cholesterol biosynthesis inhibitor RO 48-8071 suppresses growth of hormone-dependent and castration-resistant prostate cancer cells. Onco Targets Ther. 2016 May 30;9:3223-32 [Content Brief]

[3]. Liang Y, et al. Cholesterol biosynthesis inhibitors as potent novel anti-cancer agents: suppression of hormone-dependent breast cancer by the oxidosqualene cyclase inhibitor RO 48-8071. Breast Cancer Res Treat. 2014 Jul;146(1):51-62. [Content Brief]

[4]. Chuang JC, et al. Sustained and selective suppression of intestinal cholesterol synthesis by Ro 48-8071, an inhibitor of 2,3-oxidosqualene:lanosterol cyclase, in the BALB/c mouse. Biochem Pharmacol. 2014 Apr 1;88(3):351-63. [Content Brief]

Animal Administration ^[2]	Six-week-old male athymic nude mice (nu/nu) weighing 20-22 g are used in the assay. Castration-resistant PC-3 cells (5×10⁶ in 0.15 mL solution) are mixed with matrigel and RPMI-1640 medium (1/1, v/v) and injected subcutaneously into both flanks of each mouse (n=6 animals/group) and tumors allowed to develop. The tumors are measured twice per week with a digital caliper. Tumor volumes are calculated by the formula (L × W × H) × π/6. Drug treatment is started when tumor volumes reach appr 100 mm³. Mice are given daily tail vein injections of 0.1 mL solution of either 5 or 20 mg/kg Ro 48-8071 for 5 days. This is followed by an injection every other day for six additional treatments and then a final injection 2 hours prior to sacrifice. Control mice receive the same volume of phosphate-buffered saline on the same schedule. The animals are weighed and tumor volumes are measured twice weekly throughout the drug treatment period. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Morand OH, et al. Ro 48-8.071, a new 2,3-oxidosqualene:lanosterol cyclase inhibitor lowering plasma cholesterol in hamsters, squirrel monkeys, and minipigs: comparison to simvastatin. J Lipid Res. 1997 Feb;38(2):373-90. [Content Brief] [2]. Liang Y, et al. Cholesterol biosynthesis inhibitor RO 48-8071 suppresses growth of hormone-dependent and castration-resistant prostate cancer cells. Onco Targets Ther. 2016 May 30;9:3223-32 [Content Brief] [3]. Liang Y, et al. Cholesterol biosynthesis inhibitors as potent novel anti-cancer agents: suppression of hormone-dependent breast cancer by the oxidosqualene cyclase inhibitor RO 48-8071. Breast Cancer Res Treat. 2014 Jul;146(1):51-62. [Content Brief] [4]. Chuang JC, et al. Sustained and selective suppression of intestinal cholesterol synthesis by Ro 48-8071, an inhibitor of 2,3-oxidosqualene:lanosterol cyclase, in the BALB/c mouse. Biochem Pharmacol. 2014 Apr 1;88(3):351-63. [Content Brief]

Animal Administration
^[2]

Six-week-old male athymic nude mice (nu/nu) weighing 20-22 g are used in the assay. Castration-resistant PC-3 cells (5×10⁶ in 0.15 mL solution) are mixed with matrigel and RPMI-1640 medium (1/1, v/v) and injected subcutaneously into both flanks of each mouse (n=6 animals/group) and tumors allowed to develop. The tumors are measured twice per week with a digital caliper. Tumor volumes are calculated by the formula (L × W × H) × π/6. Drug treatment is started when tumor volumes reach appr 100 mm³. Mice are given daily tail vein injections of 0.1 mL solution of either 5 or 20 mg/kg Ro 48-8071 for 5 days. This is followed by an injection every other day for six additional treatments and then a final injection 2 hours prior to sacrifice. Control mice receive the same volume of phosphate-buffered saline on the same schedule. The animals are weighed and tumor volumes are measured twice weekly throughout the drug treatment period.

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

参考文献

[1]. Morand OH, et al. Ro 48-8.071, a new 2,3-oxidosqualene:lanosterol cyclase inhibitor lowering plasma cholesterol in hamsters, squirrel monkeys, and minipigs: comparison to simvastatin. J Lipid Res. 1997 Feb;38(2):373-90. [Content Brief]

[2]. Liang Y, et al. Cholesterol biosynthesis inhibitor RO 48-8071 suppresses growth of hormone-dependent and castration-resistant prostate cancer cells. Onco Targets Ther. 2016 May 30;9:3223-32 [Content Brief]

[3]. Liang Y, et al. Cholesterol biosynthesis inhibitors as potent novel anti-cancer agents: suppression of hormone-dependent breast cancer by the oxidosqualene cyclase inhibitor RO 48-8071. Breast Cancer Res Treat. 2014 Jul;146(1):51-62. [Content Brief]

[4]. Chuang JC, et al. Sustained and selective suppression of intestinal cholesterol synthesis by Ro 48-8071, an inhibitor of 2,3-oxidosqualene:lanosterol cyclase, in the BALB/c mouse. Biochem Pharmacol. 2014 Apr 1;88(3):351-63. [Content Brief]

Ro 48-8071 fumarate 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	1.7717 mL	8.8583 mL	17.7167 mL	44.2917 mL
	5 mM	0.3543 mL	1.7717 mL	3.5433 mL	8.8583 mL
	10 mM	0.1772 mL	0.8858 mL	1.7717 mL	4.4292 mL
	15 mM	0.1181 mL	0.5906 mL	1.1811 mL	2.9528 mL
	20 mM	0.0886 mL	0.4429 mL	0.8858 mL	2.2146 mL
	25 mM	0.0709 mL	0.3543 mL	0.7087 mL	1.7717 mL
	30 mM	0.0591 mL	0.2953 mL	0.5906 mL	1.4764 mL
	40 mM	0.0443 mL	0.2215 mL	0.4429 mL	1.1073 mL
	50 mM	0.0354 mL	0.1772 mL	0.3543 mL	0.8858 mL
	60 mM	0.0295 mL	0.1476 mL	0.2953 mL	0.7382 mL
	80 mM	0.0221 mL	0.1107 mL	0.2215 mL	0.5536 mL
H₂O	100 mM	0.0177 mL	0.0886 mL	0.1772 mL	0.4429 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ro 48-8071189197-69-1OthersInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

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营业执照（三证合一）

Ro 48-8071 fumarate

Customer Review

Other Forms of Ro 48-8071 fumarate:

MCE 顾客使用本产品发表的 11 篇科研文献