内吗啡肽 1 TQ0267
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
5 mg | 189388-22-5 | ¥398.00 | 询底价 |
10 mg | 189388-22-5 | ¥576.00 | 询底价 |
25 mg | 189388-22-5 | ¥1,150.00 | 询底价 |
Product Introduction
Bioactivity
英文名: Endomorphin 1
描述: Endomorphin 1 是一种高亲和力和选择性的 μ-阿片受体激动剂,对 kappa3 结合位点具有合理的亲和力 ,Ki 为 20 到 30 nM 之间。
激酶实验: 125I-Endomorphin 1 or 125I-Endomorphin 2 binding (0.2 nM) is performed in potassium phosphate buffer (50 mM, pH 7.4; 0.5 mL) with MgCl2 (5 mM) at a tissue concentration of 10 mg wet weight/mL for brains or 0.06 mg protein/mL for MOR-1/CHO cells. Specific binding is determined in the presence and absence of either 1 μM of the corresponding unlabeled peptide. The entire mixture is then incubated at 25°C for 1 hr and filtered over no. 32 glass fiber filters which have been presoaked for 1 hr in 0.5% polyethyleneimine and washed twice with ice-cold Tris buffer using a Brandel cell harvester. The filters are then counted on a Packard Cobra gamma counter. The other opioid receptor binding assays are performed.
动物实验: Groups of mice are treated i.c.v. with Endomorphin 1 (12 μg) or Endomorphin 2 (3 μg) 15 min before a 0.5-cc charcoal meal (2.5% gum tragacanth,10% activated charcoal in water). The mice are killed 30 min later and the distance the charcoal traveled is measured.
体外活性: Endomorphin是一种内源性阿片肽,也是两种Endomorphins之一。它是μ-阿片受体的高亲和力、高选择性激动剂,并且与Endomorphin 2一同作用。Endomorphin 1和Endomorphin 2都能强效地竞争μ1与μ2受体位点。Endomorphins对delta或kappa1结合位点的亲和力很低,其Ki值均大于500 nM。
体内活性: Endomorphin 1和Endomorphin 2均为有效的镇痛剂,其效果分别在10分钟和15分钟达到顶峰。所有后续研究均在达到最大效应时进行。这两种化合物在脊髓上方和脊髓内均完全活跃,且没有出现效应上限。Endomorphin 1和Endomorphin 2的作用特征与吗啡相似。在对CD-1小鼠产生超过70%镇痛效果的剂量下,这两种化合物在CXBK小鼠中均无镇痛活性。
存储条件: keep away from moisturePowder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: H2O : 24 mg/mL (39.3 mM)
关键字: inhibit | Endomorphin1 | Opioid Receptor | Inhibitor | Endomorphin 1
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相关库: Anti-Neurodegenerative Disease Compound Library | Neurotransmitter Receptor Compound Library | Anti-Parkinson's Disease Compound Library | Membrane Protein-targeted Compound Library | GPCR Compound Library | Peptide Compound Library | Human Endogenous Metabolite Compound Library Plus | Natural Product Library for HTS | NO PAINS Compound Library | Natural Product Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途