GlpBio

Endomorphin-2

目录号: GC10059纯度: >98%同义词: 内吗啡肽 2
COASDSData Sheet
Endomorphin-2是一种高亲和力、高选择性的μ-阿片受体激动剂（Ki = 0.69nM）。
Endomorphin-2
Cas No.: 141801-26-5
规格价格库存数量操作
5mg¥640.00现货
1
10mg¥1,040.00现货
1
25mg¥2,240.00现货
1
10mM (in 1mL Water)¥966.00现货
1
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产品描述 Description

Endomorphin-2 is a high-affinity and highly selective agonist of the μ-opioid receptor (Ki = 0.69nM) [1]. Endomorphin-2 activates MOR, blocking calcium channels and enhancing potassium channel opening on neurons, thereby inhibiting neural activity and achieving analgesic effects [2-3]. Endomorphin-2 is primarily used in the study of chronic pain [4].

In Wistar rats, intrahypothalamic injection of Endomorphin-2 (0.50-0.75μmol/kg; intrahypothalamic injection; single injection) induced a significant dose-related increase in food intake [5]. In CD1 mice, intraventricular injection of Endomorphin-2 (0.3-30μg; 10μL; intraventricular injection; single injection) can dose-dependently shorten the immobility time of animals in the TST test [6].

References:
[1]. Dvoracsko S, Stefanucci A, Novellino E, et al. The design of multitarget ligands for chronic and neuropathic pain[J]. Future medicinal chemistry, 2015, 7(18): 2469-2483.
[2]. Horvath G. Endomorphin-1 and endomorphin-2: pharmacology of the selective endogenous μ-opioid receptor agonists[J]. Pharmacology & therapeutics, 2000, 88(3): 437-463.
[3]. Chen Y B, Huang F S, Fen B, et al. Inhibitory effects of endomorphin-2 on excitatory synaptic transmission and the neuronal excitability of sacral parasympathetic preganglionic neurons in young rats[J]. Frontiers in cellular neuroscience, 2015, 9: 206.
[4]. Wolfe D, Hao S, Hu J, et al. Engineering an endomorphin-2 gene for use in neuropathic pain therapy[J]. PAIN®, 2007, 133(1-3): 29-38.
[5]. Brunetti L, Ferrante C, Orlando G, et al. Orexigenic effects of endomorphin-2 (EM-2) related to decreased CRH gene expression and increased dopamine and norepinephrine activity in the hypothalamus[J]. Peptides, 2013, 48: 83-88.
[6]. Fichna J, Janecka A, Piestrzeniewicz M, et al. Antidepressant-like effect of endomorphin-1 and endomorphin-2 in mice[J]. Neuropsychopharmacology, 2007, 32(4): 813-821.

Endomorphin-2是一种高亲和力、高选择性的μ-阿片受体激动剂（Ki = 0.69nM） [1]。Endomorphin-2激活MOR，阻断钙通道并增强神经元钾通道开放，从而抑制神经活动并达到镇痛作用 [2-3]。Endomorphin-2主要用于慢性疼痛的研究 [4]。

在Wistar大鼠中，下丘脑注射Endomorphin-2（0.50-0.75μmol/kg；下丘脑注射；单次注射）可显著增加大鼠的食物摄入量 [5]。在CD1小鼠中，脑室内注射Endomorphin-2（0.3-30μg；10μL；脑室内注射；单次注射）可剂量依赖性地缩短动物在TST试验中的静止时间 [6]。

实验参考方法 Experimental Reference Method

Animal experiment [1]:

Animal models

Wistar rats

Preparation Method

Sixty-four rats were anesthetized with chloral hydrate (400mg/kg, i.p.), treated with ketoprofen (1.4mg/kg), and fixed in a stereotaxic apparatus. After midline incision and local lidocaine (2%), a 21-gauge stainless steel cannula (1.7cm) was implanted into the arcuate nucleus (ARC; AP −3mm from bregma, DV −7mm) and secured with screws and dental cement. A sterile obturator was used to prevent occlusion. Postoperatively, rats received s.c. saline (1mL), 5% glucose (1mL), and piperacillin (30mg/kg, i.p.) and were monitored for 72h until recovery. At 72h, 10µL of drug/vehicle was microinjected into the ARC at 9:00 AM: Endomorphin-2 (0.50–0.75µmol/kg) or Endomorphin-2 (0.50µmol/kg) plus β-funaltrexamine (0.20µmol/kg). Injections were performed via a 10µL syringe connected to the cannula.

Dosage form

0.50-0.75μmol/kg; intrahypothalamic injection; single injection

Applications

Compared to vehicle, intrahypothalamic injection of Endomorphin-2 induced a significant dose-related increase in food intake, as evaluated 24h after treatment.

References:
[1]. Brunetti L, Ferrante C, Orlando G, et al. Orexigenic effects of endomorphin-2 (EM-2) related to decreased CRH gene expression and increased dopamine and norepinephrine activity in the hypothalamus[J]. Peptides, 2013, 48: 83-88.

产品文档 Product Documents

Purity:>98%
COASDSData Sheet

化学性质Chemical Properties

CAS 号
141801-26-5
同义词
内吗啡肽 2
化学名
(S)-N-((S)-1-(((S)-1-amino-1-oxo-3-phenylpropan-2-yl)amino)-1-oxo-3-phenylpropan-2-yl)-1-((S)-2-amino-3-(4-hydroxyphenyl)propanoyl)pyrrolidine-2-carboxamide
SMILES
O=C([C@H]1N(C([C@H](CC(C=C2)=CC=C2O)N)=O)CCC1)N[C@H](C(N[C@H](C(N)=O)CC3=CC=CC=C3)=O)CC4=CC=CC=C4
分子式
C32H37N5O5
分子量
571.65 g/mol
溶解性
≥ 57.2mg/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