Endomorphin 1 (Synonyms: 内吗啡肽 1)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白、同位素标记物,专注于信号通路和疾病研究领域。
Endomorphin 1  (Synonyms: 内吗啡肽 1) 纯度: 99.92%

Endomorphin 1,一种高度选择性的,高亲和力的 μ-opioid 受体激动剂 (Ki: 1.11 nM),对 kappa3结合位点具有高亲和力,Ki 值为 20 到 30 nM 之间。Endomorphin 1 具有镇痛特性。

Endomorphin 1                                          (Synonyms: 内吗啡肽 1)

Endomorphin 1 Chemical Structure

CAS No. : 189388-22-5

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10 mM * 1 mL in Water ¥672 In-stock
5 mg ¥500 In-stock
10 mg ¥700 In-stock
25 mg ¥1400 In-stock
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Endomorphin 1 相关产品

相关化合物库:

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  • Bioactive Compound Library Plus
  • Peptide Library

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生物活性

Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties[1][2][4].

IC50 & Target

μ Opioid Receptor/MOR

1.11 nM (Ki)

体外研究
(In Vitro)

Endomorphin 1 inhibits Forskolin (HY-15371) (1 μM) stimulated cyclic AMP formation with a pIC50 value of 8.03 in In CHOμ cells[5].
Endomorphin 1 (1-10 μM) increases interleukin-8 secretion in Caco-2 cells[6].
Endomorphin 1 (1 μM) inhibits excitatory transmission in adult rat substantia gelatinosa neurons[7].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Endomorphin 1 相关抗体:

体内研究
(In Vivo)

Endomorphin 1 (i.c.v.) shows antinociceptive properties in mice, with an ED50 value of 6.16 nM[2].
Endomorphin 1 (50 μg/kg, i.v.) alleviates myocardial ischemia/reperfusion injury (MIRI) by inhibiting the inflammatory response[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ICR mice[2].
Dosage: 6.16 nM (ED50)
Administration: Intracerebroventricularly (i.c.v.) injection
Result: Inhibited dose-dependently the tail-flick response.
Animal Model: Rats[3].
Dosage: 50 μg/kg
Administration: Intravenously following LAD ligation for 25 min, subsequently the LAD was reperfused for 120 min.
Result: Alleviated MIRI by reducing the production of free radicals.
Dncreased LDH and CK-MB activities.
Increased SOD activity and decreased MDA content.
Decreased IL-6 and TNF-α plasma content.

分子量

610.70

Formula

C34H38N6O5

CAS 号

189388-22-5

性状

固体

颜色

White to off-white

Sequence

Tyr-Pro-Trp-Phe-NH2

Sequence Shortening

YPWF-NH2

中文名称

内吗啡肽 1

结构分类
  • Alkaloids
  • Pyrrole Alkaloids
  • Alkaloids
  • Indole Alkaloids
  • Phenols
  • Monophenols
  • Others
初始来源
  • 内源性代谢物
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture and light, under nitrogen

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 50 mg/mL (81.87 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6375 mL 8.1873 mL 16.3747 mL
5 mM 0.3275 mL 1.6375 mL 3.2749 mL
10 mM 0.1637 mL 0.8187 mL 1.6375 mL

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* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)。-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。

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This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

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体积 (start)

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动物溶解方案

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给药剂量

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纯度 & 产品资料

纯度: 99.92%

Data Sheet (610 KB) SDS (252 KB)

COA (203 KB) HNMR (353 KB) LCMS (260 KB) 元素分析报告 (220 KB)

产品使用指南 (1538 KB)

参考文献
  • [1]. Goldberg IE, et al. Pharmacological characterization of endomorphin-1 and endomorphin-2 in mouse brain. J Pharmacol Exp Ther. 1998 Aug;286(2):1007-13.  [Content Brief]

    [2]. Tseng LF. The antinociceptive properties of endomorphin-1 and endomorphin-2 in the mouse. Jpn J Pharmacol. 2002 Jul;89(3):216-20.  [Content Brief]

    [3]. Zhang WP, et al. Effects of endomorphin-1 postconditioning on myocardial ischemia/reperfusion injury and myocardial cell apoptosis in a rat model. Mol Med Rep. 2016 Oct;14(4):3992-8.  [Content Brief]

    [4]. Koda Y, et al. Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides. Bioorg Med Chem. 2008 Jun 1;16(11):6286-96.  [Content Brief]

    [5]. Harrison C, et al. The effects of endomorphin-1 and endomorphin-2 in CHO cells expressing recombinant mu-opioid receptors and SH-SY5Y cells. Br J Pharmacol. 1999 Sep;128(2):472-8.  [Content Brief]

    [6]. Neudeck BL, et al. Endomorphin-1 alters interleukin-8 secretion in Caco-2 cells via a receptor mediated process. Immunol Lett. 2002 Dec 3;84(3):217-21.  [Content Brief]

    [7]. Fujita T, et al. Inhibition by endomorphin-1 and endomorphin-2 of excitatory transmission in adult rat substantia gelatinosa neurons. Neuroscience. 2006;139(3):1095-105.  [Content Brief]

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