Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CYM2503 是 GAL2 受体的正变构调节剂 (PAM),可在体外增强甘丙肽诱导的 IP1 产生。它对受体的正构甘丙肽结合位点没有亲和力(通过其无法置换碘化甘丙肽或自行诱导 IP1 积累来衡量)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 623 | 现货 | ||
5 mg | ¥ 1,530 | 现货 | ||
10 mg | ¥ 2,450 | 现货 | ||
25 mg | ¥ 4,870 | 现货 | ||
50 mg | ¥ 7,780 | 现货 | ||
100 mg | ¥ 9,870 | 现货 |
产品描述 | CYM2503 is a positive allosteric modulator (PAM) of the GAL2 receptor that potentiates galanin-induced IP1 production in vitro. It has no affinity for the orthosteric galanin binding site of the receptor (as measured by its inability to displace iodinated galanin, or to induce IP1 accumulation on its own). |
体外活性 | CYM2503 potentiated the galanin-stimulated IP1 accumulation in HEK293 cells stably expressing GalR2 receptor, whereas it exhibited no detectable affinity for the (125)I galanin-binding site of GalR2 receptor, an effect consistent with that of a positive allosteric modulator. |
体内活性 | In the rat Li-pilocarpine status epilepticus model, CYM2503, injected intraperitoneally, increased the latency to first electrographic seizure and the latency to first stage 3 behavioral seizure, decreased the latency to the establishment of status epilepticus, and dramatically decreased the mortality.?In a Li-pilocarpine seizure model in mice, CYM2503 increased the latency to first electrographic seizure and decreased the total time in seizure.?CYM2503 also attenuated electroshock-induced seizures in mice.?Thus, CYM2503 provides a starting point for the development of anticonvulsant therapy using the galanin R2 receptor as target. |
分子量 | 777.95 |
分子式 | C45H55N5O7 |
CAS No. | 1308833-36-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (64.27 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.2854 mL | 6.4271 mL | 12.8543 mL | 32.1357 mL |
5 mM | 0.2571 mL | 1.2854 mL | 2.5709 mL | 6.4271 mL | |
10 mM | 0.1285 mL | 0.6427 mL | 1.2854 mL | 3.2136 mL | |
20 mM | 0.0643 mL | 0.3214 mL | 0.6427 mL | 1.6068 mL | |
50 mM | 0.0257 mL | 0.1285 mL | 0.2571 mL | 0.6427 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。
CYM2503 1308833-36-4 GPCR/G Protein Neuroscience Neuropeptide Y Receptor electrographic seizure NPY receptor CYM-2503 CYM 2503 seizure inhibit Inhibitor epilepsy GalR2 inhibitor