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AC 261066

 
Catalog No.
B7574
有效的RARβ2激动剂
组合的产品项目
规格价格库存 数量
10mg
¥ 6,172.00
Ship with 10-15 days
50mg
¥ 20,850.00
Ship with 10-15 days

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A

背景

AC 261066是视黄酸受体亚型β同工型2(RARβ2)的激动剂[1][2]。该物质也称作UVI2062[3]。AC 261066在大鼠中具有良好的口服生物利用度(Foral= 52%)[4]。AC 261066对AKR1B10的IC50值为51 ± 7 μM。在酶促试验中,AC 261066高达100 μM时对AKR1B1无抑制能力[3]。

视黄酸受体(RARs,亚型α、β、γ)与维甲酸X受体(RXR α、β、γ)形成二聚体复合物,编排复杂事件,如器官稳态、免疫功能、发育和繁殖[1]。RARβ2是视黄酸受体β亚型的同工体,其对视黄酸的亲和性和生物学功能与其他同工体不同[2]。

AC 261066不可诱导RPMI 8866 B细胞对ADAM28解聚素样结构域的细胞粘附,不可阻断atRA诱导的粘附[5]。

AC 261066治疗相比DMSO对照可显著抑制N. viridescens的尾部再生过程。当这些AC 261066处理的蝾螈在21天(分析时间)移除AC 261066,放回正常养殖水体,尾部再生开始。移除AC 26l066后五周,尾部完成再生。相比正常尾部再生,背腹图案发生了改变[6]。

参考文献:
[1].  Albane le Maire, Susana lvarez, Pattabhiraman Shankaranarayanan, et al. Retinoid Receptors and Therapeutic Applications of RAR/RXR Modulators. Current Topics in Medicinal Chemistry, 2012, 12: 505-527.
[2].  Christopher R. Gardner, Belamy B. Cheung, Jessica Koach, et al. Synthesis of retinoid enhancers based on 2-aminobenzothiazoles for anti-cancer therapy. Bioorg. Med. Chem., 2012, 20: 6877-6884.
[3].  Sergio Porté, Joan Giménez, Marta Dominguez, et al. Aldo–keto reductases in retinoid metabolism: Search for substrate specificity and inhibitor selectivity. Chemico-Biological Interactions, 2013, 202(1-3):186-94.
[4].  Birgitte W. Lund, Fabrice Piu, Natalie K. Gauthier, et al. Discovery of a Potent, Orally Available, and Isoform-Selective Retinoic Acid β2 Receptor Agonist. J. Med. Chem., 2005, 48: 7517-7519.
[5].  Jarrett T. Whelan, Lei Wang, Jianming Chen, et al. Retinoids induce integrin-independent lymphocyte adhesion through RAR-α nuclear receptor activity. Biochemical and Biophysical Research Communications, 2014, 454: 537-542.
[6].  Christopher J. Carter. Identification of novel retinoid receptors and their roles in vertebrate and invertebrate nervous systems [D]. St. Catharines: Brock University, 2011.

化学属性

Physical AppearanceYellow solid
StorageStore at RT
M.Wt353.41
Cas No.870773-76-5
FormulaC17H20FNO4S
Solubility<35.34mg/ml in DMSO; <35.34mg/ml in ethanol
Chemical Name4-(4-(2-butoxyethoxy)-5-methylthiazol-2-yl)-2-fluorobenzoic acid
SDFDownload SDF
Canonical SMILESFC1=CC(C2=NC(OCCOCCCC)=C(C)S2)=CC=C1C(O)=O
运输条件 蓝冰运输或根据您的需求运输。
一般建议不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

质量控制

质量控制和MSDS

批次:

化学结构

AC 261066