Powder: -20°C for 3 years | In solvent: -80°C for 1 year
JNJ-5207852 是一种新型的非咪唑组胺 H3 受体拮抗剂,其对大鼠和人 H3 受体的 pKi 值分别为 8.9 和9.24。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 413 | 现货 | ||
2 mg | ¥ 598 | 现货 | ||
5 mg | ¥ 970 | 现货 | ||
10 mg | ¥ 1,730 | 现货 | ||
25 mg | ¥ 3,430 | 现货 | ||
50 mg | ¥ 4,980 | 现货 | ||
100 mg | ¥ 6,950 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,080 | 现货 |
产品描述 | JNJ-5207852 is a novel, non-imidazole histamine H3 receptor antagonist, with high affinity at the rat (pKi=8.9) and human (pKi=9.24) H3 receptor. |
靶点活性 | H3 receptor (rat):8.9 (pKi) , H3 receptor (human):9.24 (pKi) |
体内活性 | JNJ-5207852 is a potent dibasic amine antagonist that binds potently to rat H3 receptors (Ki=1.2?nm), and has good brain penetration. In ex vivo binding studies in mice, the compound had an ED50 of 0.13?mg?kg?1, subcutaneously. It promotes wakefulness in rodents at 10?mg?kg?1 s.c. but not at 1?mg?kg?1, and significantly, this effect was absent in H3 receptor KO mice. JNJ-10181457 is also a dibasic amine antagonist that exhibits high-affinity binding for the rat H3 receptor (Ki=7.1?nm), promoting wakefulness in rodents and reducing cataplectic attacks in narcoleptic dogs . JNJ-10181457 improved cognitive performance in SHR pups at 10?mg?kg?1[1]. |
分子量 | 316.48 |
分子式 | C20H32N2O |
CAS No. | 398473-34-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 77.5 mg/mL (244.88 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.1598 mL | 15.7988 mL | 31.5976 mL | 78.9939 mL |
5 mM | 0.632 mL | 3.1598 mL | 6.3195 mL | 15.7988 mL | |
10 mM | 0.316 mL | 1.5799 mL | 3.1598 mL | 7.8994 mL | |
20 mM | 0.158 mL | 0.7899 mL | 1.5799 mL | 3.9497 mL | |
50 mM | 0.0632 mL | 0.316 mL | 0.632 mL | 1.5799 mL | |
100 mM | 0.0316 mL | 0.158 mL | 0.316 mL | 0.7899 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。
JNJ-5207852 398473-34-2 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor sleep low JNJ5207852 Inhibitor REM toxicity JNJ 5207852 inhibit inhibitor