Powder: -20°C for 3 years | In solvent: -80°C for 1 year
A-381393 是选择性、可透过血脑屏障的多巴胺 D4受体拮抗剂,对人多巴胺 D4.4,D4.2和 D4.7受体的 Ki 分别为 1.5,1.9 和 1.6 nM,选择性是对 D1,D2,D3,D5多巴胺受体的 2700 多倍,对 5-HT2A 的选择性适中,Ki=370 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 473 | 现货 | ||
2 mg | ¥ 688 | 现货 | ||
5 mg | ¥ 1,210 | 现货 | ||
10 mg | ¥ 1,980 | 现货 | ||
25 mg | ¥ 3,660 | 现货 | ||
50 mg | ¥ 5,280 | 现货 | ||
100 mg | ¥ 7,450 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,330 | 现货 |
产品描述 | A-381393 is a selective and brain penetrate dopamine D4 receptor antagonist (Kis: 1.9/1.5/1.6 nM for human dopamine D4.2/D4.4/D4.7 receptor). |
靶点活性 | D4.2 receptor:1.9 nM (Ki, cell free), D4.4 receptor:1.5 nM (Ki, cell free), D4.7 receptor:1.6 nM (Ki, cell free) |
体外活性 | A-381393 potently bound to the membrane from cells expressing recombinant human dopamine D4.4 receptor (Ki=1.5 nM), which was 20-fold higher than that of clozapine (Ki=30.4 nM). A-381393 exhibited highly selective binding for the dopamine D4.4 receptor (>2700-fold) when compared to D1, D2, D3, and D5 dopamine receptors. A-381393 potently inhibited the functional activity of agonist-induced GTP-gamma-S binding assay and 1 microM dopamine-induced-Ca2+ flux in human dopamine D4.4 receptor-expressing cells, but not in human dopamine D2L or D3 receptor cells [1]. A-381393 blocked both c-Fos expression and ERK1/2 phosphorylation produced by PD168077. Treatment with A-381393 alone significantly reduced the amount of Fos immunoreactivity as compared to basal expression observed in vehicle-treated controls [2]. |
分子量 | 320.43 |
分子式 | C20H24N4 |
CAS No. | 726174-00-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (156.04 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.1208 mL | 15.604 mL | 31.2081 mL | 78.0202 mL |
5 mM | 0.6242 mL | 3.1208 mL | 6.2416 mL | 15.604 mL | |
10 mM | 0.3121 mL | 1.5604 mL | 3.1208 mL | 7.802 mL | |
20 mM | 0.156 mL | 0.7802 mL | 1.5604 mL | 3.901 mL | |
50 mM | 0.0624 mL | 0.3121 mL | 0.6242 mL | 1.5604 mL | |
100 mM | 0.0312 mL | 0.156 mL | 0.3121 mL | 0.7802 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。
A-381393 726174-00-1 GPCR/G Protein Neuroscience Dopamine Receptor inhibit A381393 A 381393 Inhibitor inhibitor