Liarozole R75251|cas:115575-11-6|西域试剂

Liarozole R75251,98.52%

产品编号：Bellancom-106019| CAS NO：115575-11-6| 分子式：C₁₇H₁₃ClN₄| 分子量：308.76

利奥唑（R75251；R85246）是一种咪唑衍生物和口服活性维甲酸（RA）代谢阻断剂（RAMBA）。利奥唑抑制视黄酸的细胞色素P450（CYP26）依赖性4-羟基化（IC50=7μM），导致视黄酸的组织水平增加。利奥唑具有抗肿瘤特性。

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-106019	￥2500.00	杭州北京（现货）
Bellancom-106019	￥4000.00	杭州北京（现货）
Bellancom-106019	￥8500.00	杭州北京（现货）
Bellancom-106019	￥13500.00	杭州北京（现货）
Bellancom-106019	￥0.00	杭州北京（现货）

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Liarozole R75251

产品介绍

Liarozole (R75251; R85246) 是一种咪唑衍生物和具有口服活性的维甲酸 (RA) 代谢阻断剂 (RAMBA)。Liarozole 抑制维甲酸依赖的细胞色素 P450 (CYP26) 4- 羟基化 (IC₅₀=7 μM)，导致组织维甲酸水平增加。Liarozole 具有抗肿瘤特性。

生物活性

Liarozole (R75251; R85246) is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC₅₀=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties.

体外研究

Liarozole (0.01~10 μM; 9 days; MCF-7 cells) inhibits cells proliferation.
Liarozole (1 μM; 4 days; mesenchymal cells) completely inhibits chondrogenesis^[4].

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

Cell Proliferation Assay

Cell Line:	MCF-7 cells
Concentration:	0.01~10 μM
Incubation Time:	9 days
Result:	Had an effect of 35% inhibition at 10 μM on cell proliferation.

Cell Differentiation Assay^[4]

Cell Line:	Mesenchymal cells
Concentration:	1 μM
Incubation Time:	4 days
Result:	Completely inhibited chondrogenesis.

体内研究
(In Vivo)

Liarozole (5-20 mg/kg; p.o.; 3 days) reverses the vaginal keratosis caused by estrogen stimulation^[5].
Liarozole (40 mg/kg; p.o.; 21 days) reduces tumor burden substantially^[6].

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

Animal Model:	Ovariectomized rats^[5]
Dosage:	5~20 mg/kg
Administration:	P.o.; 3 days
Result:	Reversed the vaginal keratosis caused by estrogen stimulation.

Animal Model:	SCID mice^[6]
Dosage:	40 mg/kg
Administration:	P.o.; 21 days
Result:	Inhibited tumor growth and survival.

体内研究

Liarozole (5-20 mg/kg; p.o.; 3 days) reverses the vaginal keratosis caused by estrogen stimulation^[5].
Liarozole (40 mg/kg; p.o.; 21 days) reduces tumor burden substantially^[6].

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

Animal Model:	Ovariectomized rats^[5]
Dosage:	5~20 mg/kg
Administration:	P.o.; 3 days
Result:	Reversed the vaginal keratosis caused by estrogen stimulation.

Animal Model:	SCID mice^[6]
Dosage:	40 mg/kg
Administration:	P.o.; 21 days
Result:	Inhibited tumor growth and survival.

体内研究

Liarozole (5-20 mg/kg; p.o.; 3 days) reverses the vaginal keratosis caused by estrogen stimulation^[5].
Liarozole (40 mg/kg; p.o.; 21 days) reduces tumor burden substantially^[6].

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

Animal Model:	Ovariectomized rats^[5]
Dosage:	5~20 mg/kg
Administration:	P.o.; 3 days
Result:	Reversed the vaginal keratosis caused by estrogen stimulation.

Animal Model:	SCID mice^[6]
Dosage:	40 mg/kg
Administration:	P.o.; 21 days
Result:	Inhibited tumor growth and survival.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (323.88 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2388 mL	16.1938 mL	32.3876 mL
5 mM	0.6478 mL	3.2388 mL	6.4775 mL
10 mM	0.3239 mL	1.6194 mL	3.2388 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 (protect from light)。-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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (8.10 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.10 mM，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；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (8.10 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.10 mM，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。
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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.10 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.10 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 25.0 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西域网站选购。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

参考文献

. Kuijpers AL, et al. The effects of oral liarozole on epidermal proliferation and differentiation in severe plaque psoriasis are comparable with those of acitretin. Br J Dermatol. 1998;139(3):380-389. [Content Brief]

. Lucker GP, et al. Oral treatment of ichthyosis by the cytochrome P-450 inhibitor liarozole. Br J Dermatol. 1997;136(1):71-75. [Content Brief]

. Wouters W, et al. Effects of liarozole, a new antitumoral compound, on retinoic acid-induced inhibition of cell growth and on retinoic acid metabolism in MCF-7 human breast cancer cells. Cancer Res. 1992;52(10):2841-2846. [Content Brief]

[4]. Pignatello MA, et al. Liarozole markedly increases all trans-retinoic acid toxicity in mouse limb bud cell cultures: a model to explain the potency of the aromatic retinoid (E)-4-[2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthylenyl)-1-propenyl] benzo [Content Brief]

[5]. Van Wauwe J, et al. Liarozole, an inhibitor of retinoic acid metabolism, exerts retinoid-mimetic effects in vivo. J Pharmacol Exp Ther. 1992;261(2):773-779. [Content Brief]

[6]. Stearns ME, et al. Liarozole and 13-cis-retinoic acid anti-prostatic tumor activity [published correction appears in Cancer Res 1993 Dec 1;53(23):5831]. Cancer Res. 1993;53(13):3073-3077. [Content Brief]

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产品编号(Item Number)

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Liarozole R75251,98.52%

Liarozole R75251

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