Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Asenapine Maleate (Org 5222 maleate) 是5-HT 和D2的拮抗剂,Ki 值分别为 0.03-4.0 nM, 1.3 nM。它也是抗精神病药物,用于治疗与双相 1 型障碍相关的精神分裂症和躁狂或混合发作。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 229 | 现货 | ||
10 mg | ¥ 372 | 现货 | ||
25 mg | ¥ 631 | 现货 | ||
50 mg | ¥ 970 | 现货 | ||
100 mg | ¥ 1,730 | 现货 | ||
200 mg | ¥ 2,990 | 现货 | ||
500 mg | ¥ 4,830 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 379 | 现货 |
产品描述 | Asenapine Maleate (Org 5222 maleate) is a second generation (atypical) antipsychotic agent that is taken sublingually and used in the treatment of schizophrenia and manic or mixed episodes associated with bipolar 1 disorder. Asenapine is associated with a low rate of transient and mild serum aminotransferase elevations during therapy but has not been linked to instances of clinically apparent acute liver injury. |
靶点活性 | 5-HT2B:9.75(pKi), 5-HT2C:10.46(pKi), 5-HT6:9.6(pKi), 5-HT2A:10.15(pKi), 5-HT7:9.94(pKi) |
体外活性 | Asenapine(0.01 mg/kg,i.v.)与NAc核相比,壳内优先增加多巴胺的流出量,而高剂量(0.05 mg/kg, i.v.)则无差异.在内侧前额叶皮质的锥体细胞中,Asenapine对NMDA诱导的应答有显著增强作用.在自由移动的大鼠中,Asenapine(0.05-0.2 mg/kg,皮下注射)诱导剂量依赖性CAR抑制(无逃避失败记录),且未诱发强直性昏厥.在大鼠在内侧前额叶皮质和伏隔核中,Asenapine(0.05-0.2 mg/kg,皮下注射)同时增加多巴胺流出. |
体内活性 | 相对于其D2受体亲和力,Asenapine对5-HT 2C,5-HT 2A,5-HT 2B,5-HT 7,5-HT 6,alpha2B和D3受体的亲和力更高,说明在治疗剂量下其与这些靶标联系更紧密。Asenapine是一种对5-HT 1A(7.4),5-HT1B(8.1),5-HT 2A(9.0),5-HT 2B(9.3),5-HT 2C(9.0),5-HT 6(8.0 ),5-HT 7(8.5),D2(9.1),D3(9.1),alpha2A(7.3),alpha2B(8.3),alpha2C(6.8)和H 1受体(8.4)有效的拮抗剂(pKB)。 |
激酶实验 | In vitro kinase activity: GST-FAK in vitro kinase activity is measured and compared to His-tagged FAK 411–686 using the K-LISA screening kit and poly(Glu:Tyr) (4:1) copolymer as a substrate immobilized on microtiter plates. IC50 values are determined with various concentrations of test compounds in a buffer containing 50 μM ATP and 10 mM MnCl2, 50 mM HEPES (pH 7.5), 25 mM NaCl, 0.01% BSA, and 0.1 mM Na orthovanadate for 5 min at room temperature. Serial diluted compounds are tested in triplicate. Substrate phosphorylation is measured using horseradish peroxidase-conjugated anti-pTyr antibodies with spetrophotometric color quantitation. IC50 values are determined using the Hill-Slope Model. Kinase selectivity profiling is performed by using the KinaseProfiler service. |
别名 | Org 5222 maleate, Org 5222, 马来酸阿塞那平, 阿塞那平马来酸盐 |
分子量 | 401.84 |
分子式 | C21H20ClNO5 |
CAS No. | 85650-56-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 74 mg/mL (184.2 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 | 2.4886 mL | 12.4428 mL | 24.8855 mL | 62.2138 mL |
5 mM | 0.4977 mL | 2.4886 mL | 4.9771 mL | 12.4428 mL | |
10 mM | 0.2489 mL | 1.2443 mL | 2.4886 mL | 6.2214 mL | |
20 mM | 0.1244 mL | 0.6221 mL | 1.2443 mL | 3.1107 mL | |
50 mM | 0.0498 mL | 0.2489 mL | 0.4977 mL | 1.2443 mL | |
100 mM | 0.0249 mL | 0.1244 mL | 0.2489 mL | 0.6221 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。
Asenapine Maleate 85650-56-2 GPCR/G Protein Neuroscience 5-HT Receptor inhibit Org5222 Inhibitor Org-5222 Org 5222 maleate Org 5222 Org 5222 Maleate 马来酸阿塞那平 5-hydroxytryptamine Receptor Serotonin Receptor Asenapine 阿塞那平马来酸盐 inhibitor