Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MPEP 是一种选择性 mGlu5 受体拮抗剂,IC50 为 36 nM,有抗焦虑和抗抑郁活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 119 | 现货 | ||
2 mg | ¥ 159 | 现货 | ||
5 mg | ¥ 247 | 现货 | ||
10 mg | ¥ 413 | 现货 | ||
25 mg | ¥ 787 | 现货 | ||
50 mg | ¥ 1,380 | 现货 | ||
100 mg | ¥ 2,230 | 现货 | ||
200 mg | ¥ 3,330 | 现货 | ||
500 mg | ¥ 5,330 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 253 | 现货 |
产品描述 | MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors. |
靶点活性 | mGluR5:36 nM |
体外活性 | MPEP has no appreciable agonist or antagonist activity at the closely related recombinant human mGlu1b receptor expressed in CHO-K1 cells or a purinoreceptor endogenously expressed in L(tk-) cells up to concentrations of 100 μM. Furthermore, MPEP shows no appreciable agonist or antagonist activity in cAMP accumulation or [35S]-GTPγS binding assays at the recombinant human group II and III metabotropic receptors (human mGlu2, -3, -4a, -6, -7b, -8a) as well as the human NMDA (NMDAR1A/2A, -1A/2B), rat AMPA (GluR3) and human kainate (GluR6) receptor subtypes. In slices of rat neonatal hippocampus, striatum, and cortex but not cerebellum, MPEP inhibits DHPG-stimulated PI hydrolysis with IC50 of 8.0 nM, 20.5 nM, and 17.9 nM, respectively. [1] MPEP positively modulates the hmGluR4 in a recombinant expression system, and the effect of MPEP is fully dependent on the activation of the orthosteric agonist L-AP4. [3] |
体内活性 | When microiontophoretically applied into the brain of rats, MPEP reduces DHPG-induced excitations but not the excitations induced by AMPA. Following intravenous administration, MPEP produces a dose-dependent inhibition of DHPG-induced but not AMPA-induced excitations with a rapid onset of action. Oral administration of MPEP also exhibits excellent anti-hyperalgesic activity in the Complete Freund's Adjuvant and turpentine models of inflammatory pain. [1] MPEP (1-30 mg/kg) induces anxiolytic-like effects in the conflict drinking test and the elevated plus-maze test in rats as well as in the four-plate test in mice. MPEP (1-20 mg/kg) shortens the immobility time in a tail suspension test in mice, but it is inactive in the behavioural despair test in rats. MPEP has no effect on locomotor activity or motor coordination. [2] MPEP significantly reduces fmr1 but not wild-type center square entries and duration. In open field tests, MPEP reduces fmr1tm1Cgr center field behavior to one indistinguishable from wild-type. MPEP produces a significant reduction of total locomotor activity in three of four groups tested, at both 10 mg/kg and 30 mg/kg. [4] |
分子量 | 193.24 |
分子式 | C14H11N |
CAS No. | 96206-92-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 37 mg/mL (191.5 mM)
Ethanol: 37 mg/mL (191.5 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 5.1749 mL | 25.8746 mL | 51.7491 mL | 129.3728 mL |
5 mM | 1.035 mL | 5.1749 mL | 10.3498 mL | 25.8746 mL | |
10 mM | 0.5175 mL | 2.5875 mL | 5.1749 mL | 12.9373 mL | |
20 mM | 0.2587 mL | 1.2937 mL | 2.5875 mL | 6.4686 mL | |
50 mM | 0.1035 mL | 0.5175 mL | 1.035 mL | 2.5875 mL | |
100 mM | 0.0517 mL | 0.2587 mL | 0.5175 mL | 1.2937 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。
MPEP 96206-92-7 Neuroscience GluR Metabotropic glutamate receptors inhibit mGluR Inhibitor inhibitor