Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dimemorfan phosphate (3,17-dimethylmorphinan) 是 sigma 1 受体激动剂,用作强效镇咳药。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 113 | 现货 | ||
10 mg | ¥ 153 | 现货 | ||
25 mg | ¥ 233 | 现货 | ||
50 mg | ¥ 328 | 现货 | ||
100 mg | ¥ 538 | 现货 |
产品描述 | Dimemorfan phosphate (3,17-dimethylmorphinan) is a sigma 1 receptor agonist. Dimemorfan phosphate is used as a potent antitussive. |
靶点活性 | σ1 receptor:150 nM(Ki) |
体外活性 | Dimemorfan (5-20 μM) inhibits both fMLP- and PMA-induced ROS production in a concentration-dependent manner and is relatively more potent in inhibiting fMLP-induced ROS production with an IC50 value of 7.0 μM. Dimemorfan (10-50 μM) does not display significant activity in scavenging free radicals by xanthine/xanthine oxidase system. Dimemorfan significantly suppressed Mac-1 upregulation both in PMA- and fMLP-activated groups. Dimemorfan (10-20 μM) significantly suppresses LPS-induced ROS and NO production, suppresses LPS-induced iNOS protein expression, and both the percentage of the positively stained population and the MCF intensities of MCP-1 and TNF-α in BV2 cytosol. Dimemorfan (20 μM) significantly blocks the degradation of cytosolic Iκ-Bα and nuclear translocation of NF-κB p65 and the transcriptional activity of NF-κB. |
体内活性 | Dimemorfan (6.25 or 12.5 mg/kg, s.c.) significantly attenuates the BAY k-8644-induced convulsive behaviors, in a dose-related manner (6.25 mg/kg dimemorfan+BAY k-8644 or 12.5 mg/kg dimemorfan+BAY k-8644 versus Saline+BAY k-8644, P<0.05 and P<0.01, respectively). Dimemorfan significantly attenuates BAY k-8644-induced increases in the c-fos and c-jun protein expression in a dose-dependent manner. Dimemorfan does not significantly affect locomotor activity or produce significant circling behavior in any locomotor pattern in mice. Dimemorfan (1 and 5 mg/kg, i.p.) surpresses the incarease of the plasma levels of TNF-α in mice. The infiltration of neutrophils into lung and liver and the production of oxidative stress (EB staining) in these tissues induced by LPS is obviously inhibited by the treatment with dimemorfan. |
别名 | 二甲啡烷磷酸盐, 3,17-dimethylmorphinan |
分子量 | 353.4 |
分子式 | C18H25N.H3O4P |
CAS No. | 36304-84-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 10 mM
DMSO: Insoluble
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O | 1 mM | 2.8297 mL | 14.1483 mL | 28.2965 mL | 70.7414 mL |
5 mM | 0.5659 mL | 2.8297 mL | 5.6593 mL | 14.1483 mL | |
10 mM | 0.283 mL | 1.4148 mL | 2.8297 mL | 7.0741 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。
Dimemorfan phosphate 36304-84-4 GPCR/G Protein Sigma receptor Dimemorfan Phosphate inhibit Inhibitor 二甲啡烷磷酸盐 3,17-dimethylmorphinan Sigma Receptor Dimemorfan inhibitor