Endomorphin 1

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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。

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 (K_i: 1.11 nM)，对 kappa₃结合位点具有高亲和力，K_i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(K_i: 1.11 nM), displays reasonable affinities for kappa₃binding sites, withK_ivalue 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°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:

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

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

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。