Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Lusaperidone (R107474) 是一种有效的α2肾上腺素受体 (adrenergic receptor) 拮抗剂,是 α (2)-肾上腺素受体的潜在放射性配体,对 α2A和α2C 具有抑制作用, Ki 值分别为0.13和0.15 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,260 | 现货 | ||
5 mg | ¥ 3,170 | 现货 | ||
10 mg | ¥ 5,290 | 现货 | ||
25 mg | ¥ 7,830 | 现货 | ||
50 mg | ¥ 10,700 | 现货 | ||
100 mg | ¥ 14,500 | 现货 |
产品描述 | Lusaperidone (R107474) is a potent α2-adrenergic receptor antagonist, a potential radioligand for the α (2)-adrenergic receptor, with inhibitory effects on α2A and α2C, with Ki values of 0.13 and 0.15 nM, respectively. |
靶点活性 | α2C-adrenoceptor:0.15 nM(Ki), α2A-adrenoceptor:2.8 nM (Kb,human), α2A-adrenoceptor:0.13 nM (Ki), α2B-adrenoceptor (human):1 nM (Ki), H5-HT7 receptor:5 nM(Ki), α2C-adrenoceptor:4.4 nM (Kb,human) |
体外活性 | Lusaperidone exhibits subnanomolar affinity for α2A and α2C adrenergic receptors (Ki=0.13 and 0.15 nM, respectively) and demonstrates nanomolar affinity for hα2B adrenergic receptors and h5-HT7 receptors (Ki=1 and 5 nM, respectively). It interacts weakly (Ki values ranging between 81 and 920 nM) with dopamine-hD2L, -hD3, and -hD4, h5-HT1D-, h5-HT1F-, h5-HT2A-, h5-HT2C-, and h5-HT5A receptors. Lusaperidone, tested up to 10 μM, interacts only at micromolar concentrations or not at all with any of the other receptor or transporter binding sites tested in this study. Furthermore, Lusaperidone has been demonstrated to reverse the clonidine-induced inhibition of cyclic AMP production mediated by human α2A and α2C adrenoceptors expressed in cell lines (Kb is 2.8 and 4.4 nM, respectively) and acts as a full antagonist on both receptor subtypes[1]. |
体内活性 | Lusaperidone occupies the α2A and α2C adrenergic receptors with an ED50 of 0.014 mg/kg sc (0.009-0.019) and 0.026 mg/kg sc (0.022-0.030), respectively. The uptake of R107474 is very rapid after in vivo intravenous administration; in most tissues, including the brain, it reaches maximum concentration at 5 min after tracer injection[1]. |
别名 | R107474 |
分子量 | 359.42 |
分子式 | C22H21N3O2 |
CAS No. | 214548-46-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 1 mg/mL (2.78 mM), Sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.7823 mL | 13.9113 mL | 27.8226 mL | 69.5565 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。
Lusaperidone 214548-46-6 GPCR/G Protein Neuroscience Adrenergic Receptor R107474 Inhibitor inhibitor inhibit