Endomorphin 1 内吗啡肽 1|cas:189388-22-5|西域试剂

Endomorphin 1 内吗啡肽 1,99.92%

产品编号：Bellancom-P0185| CAS NO：189388-22-5| 分子式：C₃₄H₃₈N₆O₅| 分子量：610.70

Endomorphin 1，一种高度选择性的高亲和力μ-opioid受体激动剂，对kappa3结合位点具有高亲和力，Ki为 20 到 30 nM 之间。

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货号	价格	库存与货期
Bellancom-P0185	￥500.00	杭州北京（现货）
Bellancom-P0185	￥700.00	杭州北京（现货）
Bellancom-P0185	￥1400.00	杭州北京（现货）

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Endomorphin 1 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 the μ-opioid receptor (K_i: 1.11 nM), displays reasonable affinities for kappa₃ binding sites, with K_i value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties^[4].

体外研究

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].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	ICR mice.
Dosage:	6.16 nM (ED₅₀)
Administration:	Intracerebroventricularly (i.c.v.) injection
Result:	Inhibited dose-dependently the tail-flick response.

Animal Model:	Rats.
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	ICR mice.
Dosage:	6.16 nM (ED₅₀)
Administration:	Intracerebroventricularly (i.c.v.) injection
Result:	Inhibited dose-dependently the tail-flick response.

Animal Model:	Rats.
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.

性状

Solid

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°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。

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)

参考文献

. 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]

. 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]

. 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]

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Endomorphin 1 内吗啡肽 1,99.92%

Endomorphin 1 内吗啡肽 1

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