Powder: -20°C for 3 years | In solvent: -80°C for 1 year
JNJ42153605是一种代谢型谷氨酸2 (mGlu2) 受体的正变构调节剂,EC50值为17 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 493 | 现货 | ||
2 mg | ¥ 718 | 现货 | ||
5 mg | ¥ 1,160 | 现货 | ||
10 mg | ¥ 1,820 | 现货 | ||
25 mg | ¥ 2,970 | 现货 | ||
50 mg | ¥ 4,290 | 现货 | ||
100 mg | ¥ 5,970 | 现货 | ||
500 mg | ¥ 11,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,270 | 现货 |
产品描述 | JNJ-42153605 is a mGlu2 receptor positive allosteric modulator (EC50: 17 nM). |
靶点活性 | mGlu2:17 nM(EC50) |
体外活性 | JNJ-42153605 is assessed for its selectivity for the mGlu2 receptor. JNJ-42153605 is found to not have agonist or antagonist activity toward other mGlu receptor subtypes up to 30 μM. JNJ-42153605 exhibits high permeability with no indication for P-glycoprotein efflux[1]. |
体内活性 | JNJ-42153605 shows a central in vivo efficacy by inhibition of REM sleep state at a dose of 3 mg/kg po in the rat sleep-wake EEG paradigm, a phenomenon shown to be mGlu2 mediated. In mice, JNJ-42153605 exhibits reversed PCP-induced hyperlocomotion with an ED50 of 5.4 mg/kg sc, suggestive of antipsychotic activity. JNJ-42153605 shows a rapid rate of absorption from the gastrointestinal tract, reaching the maximal concentration after 0.5 h. Clearance in vivo is moderate to high in both rat and dog (35 and 29 mL/min/kg, respectively). Elimination halflives are on the shorter side across the species, being 2.7 h in rat and 0.8-1.1 h in dog[1]. |
分子量 | 400.44 |
分子式 | C22H23F3N4 |
CAS No. | 1254977-87-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: Slightly soluble
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-42153605 1254977-87-1 Neuroscience GluR Inhibitor Metabotropic glutamate receptors JNJ 42153605 inhibit JNJ42153605 mGluR inhibitor