Endomorphin 1 acetate
目录号 : GC67956Endomorphin 1 acetate，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 acetate 具有镇痛特性。
Cas No.:1276123-71-7
Sample solution is provided at 25 µL, 10mM.
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Endomorphin 1 acetate, 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 acetate has antinociceptive properties[1][2][4].
Endomorphin 1 acetate inhibits Forskolin (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].
Endomorphin 1 (i.c.v.) acetate shows antinociceptive properties in mice, with an ED50 value of 6.16 nM[2].
Endomorphin 1 (50 μg/kg, i.v., rats) acetate 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. |
[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.
[2]. Tseng LF. The antinociceptive properties of endomorphin-1 and endomorphin-2 in the mouse. Jpn J Pharmacol. 2002 Jul;89(3):216-20.
[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.
[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.
[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.
[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.
[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.
| Cas No. | 1276123-71-7 | SDF | Download SDF |
| 分子式 | C36H42N6O7 | 分子量 | 670.75 |
| 溶解度 | DMSO : 250 mg/mL (372.72 mM; Need ultrasonic) | 储存条件 | Store at -20°C, protect from light, stored under nitrogen |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet