Endomorphin 1 acetate|cas:1276123-71-7|西域试剂

Endomorphin 1 acetate,99.92%

产品编号：Bellancom-P0185A| CAS NO：1276123-71-7| 分子式：C₃₆H₄₂N₆O₇| 分子量：670.75

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货号	价格	库存与货期
Bellancom-P0185A	￥550.00	杭州北京（现货）
Bellancom-P0185A	￥770.00	杭州北京（现货）
Bellancom-P0185A	￥1320.00	杭州北京（现货）

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Endomorphin 1 acetate

产品介绍

Endomorphin 1 acetate，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 acetate 具有镇痛特性。

生物活性

Endomorphin 1 acetate, 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 acetate has antinociceptive properties^[4].

体外研究

Endomorphin 1 acetate 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) acetate increases interleukin-8 secretion in Caco-2 cells^[6].
Endomorphin 1 (1 μM) acetate 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.) acetate shows antinociceptive properties in mice, with an ED₅₀ value of 6.16 nM.
Endomorphin 1 (50 μg/kg, i.v., rats) acetate 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:

DMSO : 125 mg/mL (186.36 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.4909 mL	7.4543 mL	14.9087 mL
5 mM	0.2982 mL	1.4909 mL	2.9817 mL
10 mM	0.1491 mL	0.7454 mL	1.4909 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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (3.10 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.10 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.10 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.10 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.10 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.10 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。