Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Atraric acid 衍生物作为一种新的化学先导结构,用于作为 AR 拮抗剂的新型治疗化合物,可用于预防或治疗前列腺疾病。它以剂量依赖性方式抑制 PTP1B 活性,IC50 值为 51.5 uM,表明阿特拉酸具有治疗糖尿病的潜力。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
500 mg | ¥ 291 | 现货 | ||
1 g | ¥ 350 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 195 | 现货 |
产品描述 | Atraric acid derivatives as a new chemical lead structure for novel therapeutic compounds as AR antagonists, that can be used for prophylaxis or treatment of prostatic diseases. It inhibits PTP1B activity in a dose-dependent manner with IC50 values of 51.5 uM, suggest that atraric acid has potential to treat diabetes. |
靶点活性 | PTP1B:51.5 uM |
体外活性 | Androgen receptor (AR) antagonists are important compounds for the treatment of prostate cancer (PCa). The Atraric acid (AA), a natural compound, binds to the AR and acts as a specific AR antagonist. Interestingly, Atraric acid represents a novel chemical platform that could serve as a potential basis for new AR antagonists. METHODS AND RESULTS:Therefore, one objective of this study was to analyze the chemical/structural requirements for AR antagonism and to obtain predictions of where and how Atraric acid binds to the AR. Further, this study describes the chemical synthesis of 12 Atraric acid derivatives and their analysis using a combination of computational and functional assays. Functional analysis of Atraric acid derivatives indicated that none activated the AR. Both the para-hydroxyl group and the benzene ortho- and the meta-methyl groups of Atraric acid appeared to be essential to antagonize androgen-activated AR activity. Furthermore, extension of the hydrophobic side chain of Atraric acid led to slightly stronger AR antagonism. In silico data suggest that modifications to the basic Atraric acid structure change the hydrogen-bonding network with the AR ligand binding domain (LBD), so that the para-hydroxyl group of Atraric acid forms a hydrogen bond with the LBD, confirming the functional importance of this group for AR antagonism. Moreover, in silico modeling also suggested that the ortho- and meta- methyl groups of Atraric acid interact with hydrophobic residues of the ligand pocket of AR, which might explain their functional importance for antagonism. CONCLUSIONS:Thus, these studies identify the chemical groups of Atraric acid that play key roles in allowing the Atraric acid-based chemical platform to act as an AR antagonist. |
分子量 | 196.2 |
分子式 | C10H12O4 |
CAS No. | 4707-47-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 13 mg/mL (66.26 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 5.0968 mL | 25.4842 mL | 50.9684 mL | 127.421 mL |
5 mM | 1.0194 mL | 5.0968 mL | 10.1937 mL | 25.4842 mL | |
10 mM | 0.5097 mL | 2.5484 mL | 5.0968 mL | 12.7421 mL | |
20 mM | 0.2548 mL | 1.2742 mL | 2.5484 mL | 6.371 mL | |
50 mM | 0.1019 mL | 0.5097 mL | 1.0194 mL | 2.5484 mL |
中药材名称 | 中药材拉丁名 | 性 | 味 | 归经 |
土荆皮 | Pseudolarix amabilis (Nelson) Rehd. | 温 | 辛 | 肺, 脾 |
中成药名称 | 处方组成 | 主治疾病 | 中成药类型 |
止痒酊 | 白鲜皮,土荆皮,苦参 | 外用,涂擦患处,一日2~3次。 | 化湿药 |
洁身洗液 | 苦参,蛇床子,黄柏,苍术,土荆皮,花椒,野菊花 | 外用,湿疹:反复直接涂擦患处,一日2~3次,或用温开水稀释成50%溶液湿敷,一次30分钟,一日2~3次。阴道炎:稀释成5%溶液,用专用冲洗器冲洗阴道。每次5~10分钟。 | 清热药 |
甘霖洗剂 | 甘草,苦参,白鲜皮,土荆皮 | 皮肤瘙痒取本品适量,稀释20倍,外搽患处,每日3次。外阴瘙痒取本品适量,稀释10倍,冲洗外阴和阴道,再用带尾线的棉球浸稀释5倍的药液,置于阴道内,次日取出,每日一次。患者使用本品后,无需再用水冲洗。 | 清热药 |
复方清带散 | 熊胆粉,苦参,蛇床子,黄连,土荆皮,雄黄,丁香叶,儿茶,白矾 | 将药粉装入阴道喷洒器,喷洒于患部。一次一袋,一日一次。 | 清热药 |
清肤止痒酊 | 苦参,大风子,土荆皮,白鲜皮,地肤子,构树叶,何首乌,五倍子,冰片,硫磺 | 外用,取适量涂擦患处,一日2~3次。 | 清热药 |
复方清带灌注液 | 熊胆粉,苦参,蛇床子,黄连,土荆皮,雄黄,丁香叶,儿茶,白矾(煅) | 本品包装为一次使用剂量,使用前将药液摇匀,病人取仰卧位垫高臀部,将瓶颈轻轻插入阴道8~10公分,缓缓将药液挤入阴道内保留5~10分钟,每日一次,每次一支。 | 清热药 |
癣灵药水 | 土荆皮,黄柏,白鲜皮,徐长卿,苦参,石榴皮,洋金花,南天仙子,地肤子,樟脑 | N/A | 化湿药 |
洁尔阴泡腾片 | 蛇床子,艾叶,石菖蒲,薄荷,黄柏,黄芩,苦参,地肤子,茵陈,土荆皮,栀子,金银花 | 先冲洗患部后,洗净手及外阴部,取平卧位或适当体位,戴上消毒指套用手或送药器将药片送至阴道深部后穹窿处。每晚1片,严重者可早、晚各放1片,或遵医嘱。七日为一疗程。 | 清热药 |
洁尔阴洗液 | 蛇床子,艾叶,独活,石菖蒲,苍术,薄荷,黄柏,黄芩,苦参,地肤子,茵陈,土荆皮,栀子,金银花 | 外阴、阴道炎:用10%浓度洗液(即取本品10毫升加温开水至100毫升混匀),擦洗外阴,用冲洗器将10%的洁尔阴洗液送至阴道深部冲洗阴道,一日1次,七天为一疗程;接触性皮炎、湿疹:用3%浓度洗液(即取本品3毫升加冷开水至100毫升混匀)湿敷患处,皮损轻者一日2~3次,每次30~60分钟,;无溃破者,可直接用原液涂擦,一日3~4次;7天为一疗程。体股癣:用50%浓度洗液(即取本品50毫升加冷开水至100毫升混匀)涂擦患处,一日3次,21天为一疗程。 | 清热药 |
洁尔阴软膏 | 蛇床子,艾叶,独活,石菖蒲,苍术,薄荷,黄柏,黄芪,苦参,地肤子,茵陈,土荆皮,栀子,山银花 | N/A | 清热药 |
复方土槿皮酊 | 土荆皮,苯甲酸,水杨酸 | 外用,徐患处,一日1~2次。 | 化湿药 |
癣湿药水 | 土荆皮,蛇床子,大风子仁,百部,防风,当归,凤仙透骨草,侧柏叶,吴茱萸,花椒,蝉蜕,斑蝥 | 外用。擦于洗净的患处,一日3~4次;治疗灰指甲应先除去空松部分,使药易渗入。 | 活血化瘀药 |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Atraric acid 4707-47-5 Endocrinology/Hormones Metabolism Phosphatase Androgen Receptor Inhibitor inhibitor inhibit