Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Piromelatine 是褪黑激素 MT1/MT2 受体、5-HT1A 和 5-HT1D 的激动剂,也是 5-HT2B 的拮抗剂。Piromelatine 具有抗痛觉活性,对 P2X3、TRPV1 和 Nav1.7 通道有抑制作用,可用于促进睡眠、缓解疼痛、抗神经退行性疾病和抗抑郁疾病的研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 662 | 现货 | ||
5 mg | ¥ 1,380 | 现货 | ||
10 mg | ¥ 1,980 | 现货 | ||
25 mg | ¥ 3,730 | 现货 | ||
50 mg | ¥ 5,780 | 现货 | ||
100 mg | ¥ 8,130 | 现货 | ||
500 mg | ¥ 16,200 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,550 | 现货 |
产品描述 | Piromelatine is an agonist of melatonin MT1/MT2 receptors, 5-HT1A and 5-HT1D, and an antagonist of 5-HT2B.Piromelatine has antinociceptive activity with inhibitory effects on P2X3, TRPV1, and Nav1.7 channels, and can be used in studies of sleep-promoting, pain-relieving, anti-neurodegenerative, and antidepressant diseases. diseases, and can be used to improve memory deficits associated with chronic mild stress-induced lack of pleasure in rats. |
体内活性 | Piromelatine (Neu-P11) has been shown to inhibit weight gain and improve insulin sensitivity in high-fat/high-sucrose-fed (HFSD) rats. The objective of this study was to investigate the effects of piromelatine on insulin sensitivity in sleep-restricted rats. Sleep restriction was established by rotating cages intermittently for 20h thereby sleeping time of rats was limited to 4 hours per day. During 8 days of sleep restriction, rats were injected intraperitoneally with piromelatine (20mg/kg), melatonin (5mg/kg), or a vehicle. The results showed that sleep restriction increased plasma glucose, fasting insulin, total cholesterol (TC), triglycerides (TG), and oxidative stress markers while HDL-cholesterol (HDL-C) level and glucose tolerance were decreased. However, under piromelatine or melatonin treatment, the levels of plasma glucose, TG, and TC decreased and HDL-C, glucose tolerance, and antioxidative potency increased when compared with the vehicle-treated group. Piromelatine could regulate metabolic profiles and insulin sensitivity, and attenuate insulin resistance induced by sleep restriction.[3] |
别名 | NEU-P-11, NEU-P 11, NEU-P11 |
分子量 | 312.32 |
分子式 | C17H16N2O4 |
CAS No. | 946846-83-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (320.18 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.2018 mL | 16.0092 mL | 32.0184 mL | 80.0461 mL |
5 mM | 0.6404 mL | 3.2018 mL | 6.4037 mL | 16.0092 mL | |
10 mM | 0.3202 mL | 1.6009 mL | 3.2018 mL | 8.0046 mL | |
20 mM | 0.1601 mL | 0.8005 mL | 1.6009 mL | 4.0023 mL | |
50 mM | 0.064 mL | 0.3202 mL | 0.6404 mL | 1.6009 mL | |
100 mM | 0.032 mL | 0.1601 mL | 0.3202 mL | 0.8005 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。
Piromelatine 946846-83-9 GPCR/G Protein Membrane transporter/Ion channel Neuroscience P2X Receptor 5-HT Receptor MT Receptor Sodium Channel TRP/TRPV Channel NEU-P-11 NEU-P 11 NEU-P11 Inhibitor inhibitor inhibit