Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Brexpiprazole (OPC-34712) 是人5-HT1A 和多巴胺受体的部分激动剂,Ki 分别为0.12 和 0.3 nM。它也是5-HT2A 受体的拮抗剂,Ki 为 0.47 nM,可作为非典型抗精神病药。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 393 | 现货 | ||
10 mg | ¥ 566 | 现货 | ||
25 mg | ¥ 841 | 现货 | ||
50 mg | ¥ 997 | 现货 | ||
100 mg | ¥ 1,498 | 现货 | ||
200 mg | ¥ 2,515 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 463 | 现货 |
产品描述 | Brexpiprazole (OPC-34712) is a partial agonist of human 5-hydroxytryptamine (5-HT) 5-HT1A and dopamine D2 receptors. |
靶点活性 | D2L:0.3 nM(Ki), 5-HT1A:0.12 nM(Ki), Noradrenaline α1B (human):0.17 nM(Ki), 5-HT2A receptor:0.47 nM(Ki), α2C-adrenoceptor:0.59 nM(Ki) |
体外活性 | Brexpiprazole is a potent partial agonist at human 5-hydroxytryptamine (5-HT) 5-HT1A (Ki=0.12 nM) and dopamine D2L (Ki=0.3 nM) receptors, and an antagonist at 5-HT2A receptors (Ki=0.47 nM). It also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2Creceptors (Ki=0.59 nM). Furthermore, this drug displays moderate affinity for human D3, 5-HT2B and 5-HT7 receptors, as well as α1A, and α1D adrenergic receptors. Brexpiprazole potentiated NGF-induced neurite outgrowth in PC12 cells. It could significantly potentiate the effects of fluoxetine (or paroxetine) on neurite outgrowth[1]. |
体内活性 | Brexpiprazole is able to ameliorate PCP- 191 induced cognitive deficits in mice, via 5-HT1A receptors[2]. |
细胞实验 | 2.5 ng/ml of NGF(nerve growth factor) is used to study the potentiating effects of brexpiprazole on neurite outgrowth. Twenty-four hours after plating, the medium is replaced with DMEM medium containing 0.5% FBS and 1% penicillin-streptomycin with NGF (2.5 ng/ml), with or without brexpiprazole (0.001, 0.01, 0.1 or 1.0 μM). Four days after incubation with NGF (2.5 ng/ml) with or without drugs, morphometric analysis is performed on digitized images of live cells taken under phase-contrast illumination, with an inverted microscope linked to a camera. (Only for Reference) |
别名 | 依匹哌唑, OPC-34712, 依匹唑派 |
分子量 | 433.57 |
分子式 | C25H27N3O2S |
CAS No. | 913611-97-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 23 mg/mL (53 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3064 mL | 11.5322 mL | 23.0643 mL | 57.6608 mL |
5 mM | 0.4613 mL | 2.3064 mL | 4.6129 mL | 11.5322 mL | |
10 mM | 0.2306 mL | 1.1532 mL | 2.3064 mL | 5.7661 mL | |
20 mM | 0.1153 mL | 0.5766 mL | 1.1532 mL | 2.883 mL | |
50 mM | 0.0461 mL | 0.2306 mL | 0.4613 mL | 1.1532 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。
Brexpiprazole 913611-97-9 GPCR/G Protein Neuroscience Dopamine Receptor 5-HT Receptor Adrenergic Receptor Serotonin Receptor Beta Receptor PC12 依匹哌唑 OPC-34712 5-hydroxytryptamine Receptor Inhibitor recognition deficits 依匹唑派 OPC34712 OPC 34712 antipsychotic orally active inhibit neurite outgrowth inhibitor