Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PZM21 是一种有效的选择性 μ 阿片受体激动剂,EC50值为 1.8 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 419 | 现货 | ||
5 mg | ¥ 892 | 现货 | ||
10 mg | ¥ 1,320 | 现货 | ||
25 mg | ¥ 2,160 | 现货 | ||
50 mg | ¥ 3,150 | 现货 | ||
100 mg | ¥ 4,970 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 981 | 现货 |
产品描述 | PZM21 is an effective and selective μ opioid receptor agonist (EC50: 1.8 nM). |
靶点活性 | μ opioid receptor:1.8 nM (EC50) |
体外活性 | At hERG, PZM21 has an IC50 of between 2 and 4 μM, 500- to 1,000-fold weaker than its potency as a μOR agonist. Signalling by PZM21 and other μOR agonists appears to be mediated primarily by the heterotrimeric G protein Gi/o, as its effect on cAMP levels is eliminated by pertussis toxin and no activity is observed in a calcium release assay [1]. |
体内活性 | PZM21 is a potent Gi activator with exceptional selectivity for μOR and minimal β-arrestin-2 recruitment. Unlike morphine, PZM21 is more efficacious for the affective component of analgesia versus the reflexive component and is devoid of both respiratory depression and morphine-like reinforcing activity in mice at equi-analgesic doses. PZM21 displays dose-dependent analgesia in a mouse hotplate assay, with a per cent maximal possible effect (% MPE) of 87% reached 15 min after administration of the highest dose of drug tested [1].PZM21 has a long-lasting analgesic effect on CNS mediated-pain responses, but does not cause respiratory depression and constipation, two key side effects of opioid agonists [2]. |
分子量 | 361.5 |
分子式 | C19H27N3O2S |
CAS No. | 1997387-43-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 27.5 mg/mL (76.07 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.7663 mL | 13.8313 mL | 27.6625 mL | 69.1563 mL |
5 mM | 0.5533 mL | 2.7663 mL | 5.5325 mL | 13.8313 mL | |
10 mM | 0.2766 mL | 1.3831 mL | 2.7663 mL | 6.9156 mL | |
20 mM | 0.1383 mL | 0.6916 mL | 1.3831 mL | 3.4578 mL | |
50 mM | 0.0553 mL | 0.2766 mL | 0.5533 mL | 1.3831 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。
PZM21 1997387-43-5 Endocrinology/Hormones GPCR/G Protein Neuroscience Opioid Receptor Inhibitor PZM 21 inhibit PZM-21 inhibitor