维生素A酸 T1051

Product Introduction
Bioactivity


英文名: Retinoic acid

描述: Retinoic acid (Tretinoin) 是维生素 A 的代谢产物，是一种视黄酸受体 RAR 的天然激动剂，抑制 RARα/β/γ (IC50=14 nM)。Retinoic acid 可以诱导细胞分化、减少细胞增殖和抑制肿瘤发生。

细胞实验: Retinoic acid is dissolved in DMSO and stored, and then diluted with appropriate medium before use[3]. P19 cell are induced to undergo neuronal differentiation according to established procedures. Briefly, cells are cultured on 1% agarose-coated 10 cm dishes at 3×10 5 cells/mL in α-minimal essential medium supplemented with 10% FBS. Differentiation is induced by addition of Retinoic acid (1 μM) and medium containing Retinoic acid replaced 2 days later. On day 4, cell aggregates are collected by centrifugation, separated to single cells by trypsin/EDTA treatment, replated onto poly-L-lysine-coated plates, and cultured in α-minimal essential medium supplemented with 10% FBS. On day 6, medium is replaced with neurobasal medium containing B27 supplement and 2 mM GlutaMAX. Medium is replaced every 2 days for an additional week[3].

体外活性: 方法：人单核细胞 THP-1 用 Retinoic acid (10-100 nM) 处理 24 h，使用 Western Blot 方法检测靶点蛋白表达水平。结果：Retinoic acid 处理的细胞中 RXRα 和 RARα 蛋白持续减少。[1]方法：小鼠胚胎干细胞 mESC 用 Retinoic acid (1 μM) 处理 24 h，进行基因表达微阵列分析。结果：Retinoic acid 处理后分化相关基因 Hoxb1、Hoxb2 和 Hoxb3 上调，而多能性相关基因 Oct4、Nanog、Klf4、Esrrb、Lefty1 和 Letfy2 下调。Retinoic acid 诱导ES细胞外胚层标志物表达。[2]

体内活性: 方法：为研究对小鼠齿筋膜兴奋性和抑制性神经传递的影响，将 Retinoic acid (10 mg/kg in Corn oil+5% DMSO) 单次腹腔注射给 C57BL/6J 小鼠。结果：在给予 Retinoic acid 6 h 后，背侧海马中的自发兴奋性突触后电流频率和突触数量均显著增加。Retinoic acid 介导小鼠齿状颗粒细胞中突触足蛋白依赖性化生。[3]方法：为检测对小鼠肝脏脂质代谢的影响，将 Retinoic acid (10-100 mg/kg) 皮下注射给 NMRI 小鼠，每天一次，持续四天。结果：Retinoic acid 治疗可减轻体重和肥胖。Retinoic acid 在体内将肝脏脂质代谢转变为增加分解代谢和减少脂肪生成。[4]

存储条件: keep away from direct sunlightPowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 45 mg/mL (149.78 mM)
Ethanol : 6 mg/mL (19.97 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: PPAR | inhibit | Endogenous Metabolite | RAR/RXR | Inhibitor | Retinoic acid | Retinoic acid receptors | Retinoid X receptors | Peroxisome proliferator-activated receptors | Autophagy

相关产品: Fenretinide | Acitretin | BMS453 | Talarozole | palovarotene | BMS 753 | HX 531 | Adapalene | Etodolac | AC-55649

相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | Autophagy Compound Library | Metabolism Compound Library | Target-Focused Phenotypic Screening Library | Preclinical Compound Library | Covalent Inhibitor Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途