Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Lurasidone (SM-13496) 是多巴胺 D2和5-HT7的拮抗剂,IC50值分别为 1.68 和 0.495 nM。它也是5-HT1A 受体的部分激动剂,IC50值为 6.75 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 198 | 现货 | ||
10 mg | ¥ 333 | 现货 | ||
25 mg | ¥ 565 | 现货 | ||
50 mg | ¥ 925 | 现货 | ||
100 mg | ¥ 1,430 | 现货 | ||
200 mg | ¥ 2,130 | 待询 |
产品描述 | Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7(IC50=1.68 and 0.495 nM, respectively).It also a partial agonist of 5-HT1A receptor(IC50 : 6.75 nM). |
靶点活性 | 5-HT7 receptor:0.495 nM (IC50), 5-HT1A receptor:6.75 nM (IC50), D2 receptor:1.68 nM (IC50) |
体外活性 | Lurasidone is administered once daily within the range of 40-160 mg/day for schizophrenia and 20-120 mg/day for bipolar depression, and its pharmacokinetic profile requires administration with food.?In adult healthy subjects and patients, a 40 mg dose results in peak plasma concentrations in 1-3 h, a mean elimination half-life of 18 h (mostly eliminated in the feces), and apparent volume of distribution of 6173 L;?it is approximately 99 % bound to serum plasma proteins.?Lurasidone's pharmacokinetics are approximately dose proportional in healthy adults and clinical populations within the approved dosing range, and this was also found in a clinical study of children and adolescents.?Lurasidone is principally metabolized by cytochrome P450 (CYP) 3A4 with minor metabolites and should not be coadministered with strong CYP3A4 inducers or inhibitors.?Lurasidone does not significantly inhibit or induce CYP450 hepatic enzymes[2]. |
体内活性 | In addition to its principal antagonist activity at dopamine D2 and serotonin 5-HT2A receptors, lurasidone has distinctive 5-HT7 antagonistic activity, and displays partial agonism at 5-HT1A receptors, as well as modest antagonism at noradrenergic α2A and α2C receptors.?Lurasidone is devoid of antihistaminic and anticholinergic activities[1]. |
别名 | SM-13496, 鲁拉西酮 |
分子量 | 492.68 |
分子式 | C28H36N4O2S |
CAS No. | 367514-87-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 17.83 mg/mL (36.19 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0297 mL | 10.1486 mL | 20.2972 mL | 50.7429 mL |
5 mM | 0.4059 mL | 2.0297 mL | 4.0594 mL | 10.1486 mL | |
10 mM | 0.203 mL | 1.0149 mL | 2.0297 mL | 5.0743 mL | |
20 mM | 0.1015 mL | 0.5074 mL | 1.0149 mL | 2.5371 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。
Lurasidone 367514-87-2 GPCR/G Protein Neuroscience Dopamine Receptor 5-HT Receptor SM 13496 SM-13496 SM13496 鲁拉西酮 inhibit Serotonin Receptor 5-hydroxytryptamine Receptor Inhibitor inhibitor