货号	规格	价格	上海	北京	珠海	重庆	武汉
S88547-1mg	≥98%	￥430.00 S88547-1mg ￥430.00 3-5天	0 货期：3-5天	-	-	-	-
S88547-5mg	≥98%	￥810.00 S88547-5mg ￥810.00 3-5天	0 货期：3-5天	-	-	-	-
S88547-10mg	≥98%	￥1220.00 S88547-10mg ￥1220.00 3-5天	0 货期：3-5天	-	-	-	-
S88547-50mg	≥98%	￥2910.00 S88547-50mg ￥2910.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM

靶点：

EC50: 1.8 nM (μ opioid receptor);OpioidReceptor

体外研究：

PZM21 has no detectable κOR or nociceptin receptor agonist activity-it is actually an 18 nM κOR antagonist-while it is a 500-fold weaker δOR agonist, making it a selective μOR agonist. 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

体内研究：

PZM21 is a potent Gi activator with exceptional selectivity for μOR and minimal β-arrestin-2 recruitment. PZM21 is efficacious for the affective component of analgesia versus the reflexive component and is devoid of respiratory depression 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.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

参考文献：

1. Manglik A, et al. Structure-based discovery of opioid analgesics with reduced side effects. Nature. 2016 Sep 8;537(7619):185-190. 2. Kostic M, et al. Biasing Opioid Receptors and Cholesterol as a Player in Developmental Biology. 3. Araldi D, et al. Mu-opioid Receptor (MOR) Biased Agonists Induce Biphasic Dose-dependent Hyperalgesia and Analgesia, and Hyperalgesic Priming in the Rat. Neuroscience. 2018 Oct 17;394:60-71.

溶解性：

Soluble in DMSO

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.766 ml	13.831 ml	27.662 ml
5 mM	0.553 ml	2.766 ml	5.532 ml
10 mM	0.277 ml	1.383 ml	2.766 ml
50 mM	0.055 ml	0.277 ml	0.553 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置

PZM-21

1-((S)-2-(dimethylamino)-3-(4-hydroxyphenyl)propyl)-3-((S)-1-(thiophen-3-yl)propan-2-yl)urea

参考文献

质检证书(COA)

如何获取质检证书(COA)?

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)