| CAS NO: | 253310-42-8 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 448.51 |
| Cas No. | 253310-42-8 |
| Formula | C29H24N2O3 |
| Solubility | <11.21mg/ml in DMSO |
| Chemical Name | 4-(5,5-dimethyl-8-(quinolin-3-yl)-5,6-dihydronaphthalene-2-carboxamido)benzoic acid |
| Canonical SMILES | CC1(CC=C(C2=C1C=CC(C(NC3=CC=C(C(O)=O)C=C3)=O)=C2)C4=CC5=CC=CC=C5N=C4)C |
| 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。 |
BMS 195614是RARα的选择性拮抗剂[1]，可结合RARα亚基[5]。
BMS195614，4-[[[[5,6-二氢-5,5-二甲基-8-(3-喹啉基)]-2-萘基]羰基]氨基]苯甲酸[2]，是维甲酸的拮抗剂，通过伴随地转染视黄酸受体（RAR），抑制全反式视黄酸诱导的（ATRA诱导的）视黄酸反应元件-氯霉素乙酰转移酶（RARE-CAT）报告子表达[3][4]。
视黄酸（RA）是维生素A（视黄醇）最主要的具有生物活性的衍生物（一并称作维甲酸）。视黄酸对细胞分化、脊椎动物发育和稳态有多种重要作用[6]。
BMS 195614可逆转RARα选择性激活剂AM580、AM80和BMS 194753对急性早幼粒细胞白血病细胞系NB4和HL60分化的诱导效应[1]。视黄酸（RA）（10-6 M）处理72小时可显著降低T47D乳腺癌细胞转移。但RA与BMS 195614结合不影响细胞运动[7]。在牛肌内脂肪来源的间质-血管细胞中，BMS 195614可显著减弱ATRA的抗脂肪形成作用[8]。
BMS 195614在小鼠口服给药时体内活性较差。BMS 195614口服给药1个月对精子生成无抑制作用[3]。口服BMS 195614不能抑制小鼠精子生成[9]。
参考文献：
[1]. F. Christopher Zusi, Matthew V. Lorenzi and Valerie Vivat-Hannah. Selective retinoids and rexinoids in cancer therapy and chemoprevention. Drug Discovery Today, 2002, 7(23):1165-1174.
[2]. John E. Starrett, Jr., David R. Tortolani, Muzammil M. Mansuri, et al. Bristol-Myers Squibb Co. Retinoid-like Heterocycles. US patent 5,559,248. 1996 Sep. 24.
[3]. Sanny S. W. Chung, Rebecca A. D. Cuellar, Xiangyuan Wang, et al. Pharmacological Activity of Retinoic Acid Receptor Alpha-Selective Antagonists in Vitro and in Vivo. ACS Med. Chem. Lett., 2013, 4: 446-450.
[4]. Eun Young Park, Alice Dillard, Elizabeth A. Williams, et al. Retinol Inhibits the Growth of All-Trans-Retinoic Acid–Sensitive and All-Trans-Retinoic Acid–Resistant Colon Cancer Cells through a Retinoic Acid Receptor–Independent Mechanism. Cancer Res., 2005, 65(21):9923-9934.
[5]. Dongchun Liang, Aijun Zuo, Hui Shao, et al. Retinoic Acid Inhibits CD25 Dendritic Cell Expansion and cd T-Cell Activation in Experimental Autoimmune Uveitis. Invest Ophthalmol Vis Sci., 2013, 54:3493-3503.
[6]. Pierre Chamban. A decade of molecular biology of retinoic acid receptors. FASEBJ., 1996, 10:940-954.
[7]. Flamini Marina Ines, Gauna Gisel Valeria, Sottile Mayra Lis, et al. Retinoic acid reduces migration of human breast cancer cells: role of retinoic acid receptor β. J. Cell. Mol. Med., 2014, 18(6): 1113-1123.
[8]. Nikolas Gunkel, Thorsten Meyer and John Michael Graettinger; N/A. Method of Modulating the Degree of Adipose Tissue Deposited Intramuscularly. US patent 20140094512A1. 2014 Apr. 3.
[9]. Fern E. Murdoch and Erwin Goldberg. Male contraception: Another holy grail. Bioorg. Med. Chem. Lett., 2014, 24:419-424.
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