Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BIA 10-2474 是一种长效可逆的脂肪酸酰胺水解酶抑制剂,与人类内源性大麻素系统相互作用,可增加中枢神经系统和外周组织,对大鼠大脑不同区域的 IC50值为50至70mg/kg。它用于治疗焦虑症、帕金森氏病和多发性硬化症、高血压或肥胖症的慢性疼痛。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 218 | 现货 | ||
5 mg | ¥ 496 | 现货 | ||
10 mg | ¥ 868 | 现货 | ||
25 mg | ¥ 1,620 | 现货 | ||
50 mg | ¥ 2,590 | 现货 | ||
100 mg | ¥ 4,130 | 现货 |
产品描述 | BIA 10-2474 is a long-acting reversible inhibitor of fatty acid amide hydrolase (FAAH) that increases levels of the neurotransmitter anandamide in the central nervous system and in peripheral tissues (that is, the rest of the body other than the brain and spinal cord). BIA 10-2474(BIA10-2474) interacts with the human endocannabinoid system. BIA 10-2474(BIA10-2474) was in development for the treatment of a range of different medical conditions from anxiety to Parkinson's disease, also for the treatment of chronic pain of multiple sclerosis, Y, hypertension or the treatment of obesity. |
靶点活性 | FAAH, rat brain regions:50-70mg/kg (IC50) |
体外活性 | ExVivo: BIA 10-2474 proves to be a potent FAAH inhibitor with IC50s of 50-70 mg/kg (i.p.) in various brain regions. IC50 values for brain regions are 52 (cerebellum), 67 (rest of brain), 68 (cortex), and 71 mg/kg (hypothalamus)[1]. |
体内活性 | In January 2016, severe adverse events (SAE) occurs in the Phase I Clinicalal trial using the drug BIA 10-2474 including one death. The possibilities for failure of trials such as off-target effect, dose calculation, unexpected immune response, species variation, and cumulative dose toxicity would be sought[2]. |
别名 | BIA10-2474 |
分子量 | 300.36 |
分子式 | C16H20N4O2 |
CAS No. | 1233855-46-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 4 mg/mL(13.3 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.3293 mL | 16.6467 mL | 33.2934 mL | 83.2335 mL |
5 mM | 0.6659 mL | 3.3293 mL | 6.6587 mL | 16.6467 mL | |
10 mM | 0.3329 mL | 1.6647 mL | 3.3293 mL | 8.3233 mL |
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。
BIA 10-2474 1233855-46-3 Autophagy Metabolism Neuroscience FAAH BIA 10 2474 Fatty acid amide hydrolase Inhibitor BIA10-2474 BIA 102474 inhibit inhibitor