L-Phenylalaninamide, L-tyrosyl-L-prolyl-L-tryptophyl-, acetate (1:1)
- CAS No.
- 1276123-71-7
- Chemical Name:
- L-Phenylalaninamide, L-tyrosyl-L-prolyl-L-tryptophyl-, acetate (1:1)
- Synonyms
- Endomorphin 1 acetate;L-Phenylalaninamide, L-tyrosyl-L-prolyl-L-tryptophyl-, acetate (1:1)
- CBNumber:
- CB212837388
- Molecular Formula:
- C36H42N6O7
- Molecular Weight:
- 670.77
- MDL Number:
- MOL File:
- 1276123-71-7.mol
L-Phenylalaninamide, L-tyrosyl-L-prolyl-L-tryptophyl-, acetate (1:1) Chemical Properties,Uses,Production
Uses
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].
in vivo
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. |
IC 50
μ Opioid Receptor/MOR: 1.11 nM (Ki)
References
[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. PMID:9694962
[2] Tseng LF. The antinociceptive properties of endomorphin-1 and endomorphin-2 in the mouse. Jpn J Pharmacol. 2002 Jul;89(3):216-20. DOI:10.1254/jjp.89.216
[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. DOI:10.3892/mmr.2016.5695
[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. DOI:10.1016/j.bmc.2008.04.020
[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. DOI:10.1038/sj.bjp.0702798
[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. DOI:10.1016/s0165-2478(02)00198-0
[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. DOI:10.1016/j.neuroscience.2006.01.010
L-Phenylalaninamide, L-tyrosyl-L-prolyl-L-tryptophyl-, acetate (1:1) Preparation Products And Raw materials
Raw materials
Preparation Products
L-Phenylalaninamide, L-tyrosyl-L-prolyl-L-tryptophyl-, acetate (1:1) Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32239 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 52924 | 58 | |
| Shanghai Yifei Biotechnology Co. , Ltd. | 021-65675885 18964387627 | customer_service@efebio.com | China | 11973 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 19820 | 58 |
| Adooq Bioscience LLC | 400-025-6535 | sales@adooq.cn | China | 18215 | 58 |
| Supplier | Advantage |
|---|---|
| TargetMol Chemicals Inc. | 58 |
| Aladdin Scientific | 58 |
| Shanghai Yifei Biotechnology Co. , Ltd. | 58 |
| TargetMol Chemicals Inc. | 58 |
| Adooq Bioscience LLC | 58 |
View Lastest Price from L-Phenylalaninamide, L-tyrosyl-L-prolyl-L-tryptophyl-, acetate (1:1) manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
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2025-04-29 | Endomorphin 1 acetate
1276123-71-7
|
US $37.00 / mg | 10g | TargetMol Chemicals Inc. |
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- Endomorphin 1 acetate
1276123-71-7
- US $37.00 / mg
- TargetMol Chemicals Inc.