Endomorphin-1

目录号: GP10065纯度: >98%同义词: 内吗啡肽 1

An endogenous neuropeptide and μ-opioid receptor agonist


Endomorphin-1
Cas No.: 189388-22-5
规格价格库存数量操作
25mg¥357.00现货
1
10mM (in 1mL DMSO)¥347.00现货
1

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产品描述 Description

Endomorphins are two endogenous opioid peptides. Endomorphin-1 (Tyr-Pro-Trp-Phe-NH2) and endomorphin-2 (Tyr-Pro-Phe-Phe-NH2) are tetrapeptides with the highest known affinity and specificity for the μ opioid receptor. Endomorphin-1 is located in the nucleus of the solitary tract, the periventricular hypothalamus, and the dorsomedial hypothalamus, where it is found within histaminergic neurons and may regulate sedative and arousal behaviors1. It is assumed that endomorphins are the cleavage products of a larger precursor, but this polypeptide or protein has not yet been identified. Perikarya expressing EM2-like immunoreactivity were present in the posterior hypothalamus, whereas those expressing EM1-like immunoreactivity were present in both the posterior hypothalamus and the nucleus of the solitary tract (NTS). EM1-like immunoreactivity was more widely and densely distributed throughout the brain than was EM2-like immunoreactivity, whereas EM2-like immunoreactivity was more prevalent in the spinal cord than was EM1-like immunoreactivity. endomorphins participate in modulating nociceptive and autonomic nervous system processes and responsiveness to stress.

References:
1. Greco, MA; Fuller, PM; Jhou, TC; Martin-Schild, S; Zadina, JE; Hu, Z; Shiromani, P; Lu, J (2008). "Opioidergic projections to sleep-active neurons in the ventrolateral preoptic nucleus". Brain Research 1245: 96–107.

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

Primary human fetal mixed glial/neuronal brain cell, human microglial cell

Preparation method

The solubility of this compound in DMSO is >30.6 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.1 nM

Applications

In mixed glial/neuronal cell cultures infected with HIV-1, endomorphin-1 potentiated the expression of HIV-1 in a bell-shaped dose-response manner. Endomorphin-1 (0.1 nM) consistently amplified the replication of HIV-1. In microglial cells, endomorphin-1 potentiated the expression of HIV-1, with maximal enhancement of HIV-1 expression at 10-10M.

Animal experiment [2, 3]:

Animal models

Male ICR mice, adult female Sprague–Dawley rats

Dosage form

i.c.v. injection, 5 min, 3.28 nM-16.38 nM, intrathecal injection

Application

Endomorphin-1 inhibited the tail-flick (AD50 = 6.16 nM) and hot-plate responses (AD50 = 1.94 nM) in a dose-dependent manner at 5 min after i.c.v. injection. In rats, intrathecal injection of 1:10 and 1:100 times diluted EM1 antiserum significantly decreased the effect of 2 Hz electroacupuncture analgesia.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Peterson P K, Gekker G, Hu S, et al. Endomorphin-1 potentiates HIV-1 expression in human brain cell cultures: implication of an atypical μ-opoid receptor[J]. Neuropharmacology, 1999, 38(2): 273-278.

[2]. Tseng L F, Narita M, Suganuma C, et al. Differential antinociceptive effects of endomorphin-1 and endomorphin-2 in the mouse[J]. Journal of Pharmacology and Experimental Therapeutics, 2000, 292(2): 576-583.

[3]. Han Z, Jiang Y H, Wan Y, et al. Endomorphin-1 mediates 2 Hz but not 100 Hz electroacupuncture analgesia in the rat[J]. Neuroscience letters, 1999, 274(2): 75-78.

产品文档 Product Documents

化学性质Chemical Properties

CAS 号
189388-22-5
同义词
内吗啡肽 1
化学名
(2S)-1-[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]-N-[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]pyrrolidine-2-carboxamide
SMILES
C1CC(N(C1)C(=O)C(CC2=CC=C(C=C2)O)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CC5=CC=CC=C5)C(=O)N
分子式
C34H38N6O5
分子量
610.67 g/mol
溶解性
≥ 30.55mg/mL in DMSO
保存条件
Desiccate at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol