Liarozole dihydrochloride|1883548-96-6|(R75251 dihydrochloride)-陌孚医药/Medlife

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Liarozole dihydrochloride (Synonyms: R75251 dihydrochloride)

目录号: PL10802 纯度: ≥99.0%

CAS No. :1883548-96-6

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中文名称	Liarozole dihydrochloride
英文名称	Liarozole dihydrochloride
英文别名	Liarozole (dihydrochloride);Liarozole dihydrochloride;6-((3-Chlorophenyl)(1H-imidazol-1-yl)methyl)-1H-benzo[d]imidazole dihydrochloride;5-[(3-Chlorophenyl)-1H-imidazol-1-ylmethyl]-1H-benzimidazole dihydrochloride
Cas No.	1883548-96-6
分子式	C₁₇H₁₅Cl₃N₄
分子量	381.69
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Liarozole (R75251) dihydrochloride 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 dihydrochloride 抑制细胞色素 P450 (CYP26) 依赖的维甲酸 4- 羟基化 (IC₅₀=7 μM)，导致组织 RA 水平增加。Liarozole dihydrochloride 具有抗肿瘤活性。

生物活性

Liarozole (R75251) dihydrochloride is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole dihydrochloride inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of RA (IC 50 =7 μM), resulting in increased tissue levels of RA. Liarozole dihydrochloride shows antitumoral properties.

性状

Solid

IC50 & Target[1][2]

CYP26 7 μM (IC50)

体外研究(In Vitro)

Liarozole dihydrochloride (0.01~10 μM; 9 days; MCF-7 cells) inhibits cells proliferation.
Liarozole dihydrochloride (1 μM; 4 days; mesenchymal cells) completely inhibits chondrogenesis. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay

体内研究(In Vivo)

Liarozole dihydrochloride (5-20 mg/kg; p.o.) reverses the vaginal keratosis caused by estrogen stimulation.
Liarozole dihydrochloride (40 mg/kg; p.o.) reduces tumor burden substantially. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

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

溶解度数据	In Vitro: H₂O : ≥ 50 mg/mL (131.00 mM)DMSO : 50 mg/mL (131.00 mM; Need ultrasonic)

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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