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Endomorphin 1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Endomorphin 1图片
CAS NO:189388-22-5
包装与价格:
包装价格(元)
10 mM * 1 mL in Water电议
5mg电议
10mg电议
25mg电议

产品名称
内吗啡肽 1
产品介绍
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。
生物活性

Endomorphin 1, a high affinity, highly selective agonist of theμ-opioid receptor(Ki: 1.11 nM), displays reasonable affinities for kappa3binding sites, withKivalue 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 inhibitsForskolin(HY-15371) (1 μM) stimulated cyclic AMP formation with a pIC50value 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].

体内研究
(In Vivo)

Endomorphin 1 (i.c.v.) shows antinociceptive properties in mice, with an ED50value of 6.16 nM[2].
Endomorphin 1 (50 μg/kg, i.v.) alleviates myocardial ischemia/reperfusion injury (MIRI) by inhibiting the inflammatory response[3].

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

性状

Solid

Formula

C34H38N6O5

CAS 号

189388-22-5

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
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°C2 years
-20°C1 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: 

H2O : 25 mg/mL(40.94 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.6375 mL8.1873 mL16.3747 mL
5 mM0.3275 mL1.6375 mL3.2749 mL
10 mM0.1637 mL0.8187 mL1.6375 mL
*

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light, under nitrogen)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。