CAS NO: | 870773-76-5 |
包装 | 价格(元) |
10mg | 电议 |
50mg | 电议 |
Physical Appearance | Yellow solid |
Storage | Store at RT |
M.Wt | 353.41 |
Cas No. | 870773-76-5 |
Formula | C17H20FNO4S |
Solubility | <35.34mg/ml in DMSO;<35.34mg/ml in ethanol |
Chemical Name | 4-(4-(2-butoxyethoxy)-5-methylthiazol-2-yl)-2-fluorobenzoic acid |
Canonical SMILES | FC1=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 | 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。 |
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.