Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MDL 29951 是一种新颖的 nMDA receptor 拮抗剂,能够抑制体内体外甘氨酸 ([3H]glycine) 的结合,Ki=0.14 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 578 | 现货 | ||
2 mg | ¥ 839 | 现货 | ||
5 mg | ¥ 1,380 | 现货 | ||
10 mg | ¥ 2,470 | 现货 | ||
25 mg | ¥ 4,190 | 现货 | ||
50 mg | ¥ 5,970 | 现货 | ||
100 mg | ¥ 8,260 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,380 | 现货 |
产品描述 | MDL-29951 is a novel glycine antagonist of NMDA receptor activation. |
靶点活性 | NMDA:0.14 μM |
体外活性 | MDL 100,748 and MDL 29,951 are approximately 2000-fold selective for the glycine binding site relative to the glutamate recognition sites[1]. MDL-29951 is found to inhibit the human F16Bpase under these conditions (IC50=2.5 μM). MDL-29951 inhibits the human liver (IC50=2.5 μM), porcine kidney (IC50=1.0 μM), and rabbit liver (IC50=0.21 μM) isoforms of the enzyme, but is significantly less potent against the rat liver isoform (IC50=11 μM)[2]. The MDL29951-activated receptor exhibits other activities associated with GPCR-mediated signaling, including G protein-dependent activation of extracellular signal-regulated kinase 1 and 2 (ERK1/2) and recruitment of β-arrestin. As with recombinant cell systems, MDL29951 promotes Ca2+ signaling responses and inhibition of cyclic adenosine monophosphate (cAMP) accumulation in rat oligodendrocyte precursor cells during the period of peak GPR17 abundance. Effects of MDL29951 are markedly reduced in cells with low GPR17 abundance and are blocked by pranlukast[3]. |
激酶实验 | [3H]JCPP (30.7 Ci/mmol) binding assays are conducted in minivials, incubated for 15 mm at 25°C in 1 mL of 50 mM Tris-HC1 (pH 7.4) containing 10 nM [3H]JCPP, 200 g of membrane protein and unlabeled ligands as indicated. Nonspecific binding is defined using 1 mM L-glutamate. Bound ligand is separated by centrifugation. Specific binding accounted for approximately 80% of total binding. |
分子量 | 302.11 |
分子式 | C12H9Cl2NO4 |
CAS No. | 130798-51-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (165.5 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.3101 mL | 16.5503 mL | 33.1005 mL | 82.7513 mL |
5 mM | 0.662 mL | 3.3101 mL | 6.6201 mL | 16.5503 mL | |
10 mM | 0.331 mL | 1.655 mL | 3.3101 mL | 8.2751 mL | |
20 mM | 0.1655 mL | 0.8275 mL | 1.655 mL | 4.1376 mL | |
50 mM | 0.0662 mL | 0.331 mL | 0.662 mL | 1.655 mL | |
100 mM | 0.0331 mL | 0.1655 mL | 0.331 mL | 0.8275 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。
MDL-29951 130798-51-5 Membrane transporter/Ion channel Neuroscience NMDAR iGluR Ionotropic glutamate receptors Inhibitor MDL 29951 MDL29951 inhibit inhibitor