Endomorphin 1
Based on 3 publication(s) in Google Scholar
Endomorphin 1, 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 has antinociceptive properties.
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- Purity: 99.92%
- CAS No.: 189388-22-5
- 화학식: C34H38N6O5
- 분자량:610.70
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보관:
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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Endomorphin 1
MoreAll Opioid Receptor Isoforms
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Biological Activity
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μ Opioid Receptor/MOR 1.11 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.001 nM
Compound: 1, Endomorphin-1
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Activity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay
Activity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay
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[PMID: 17266203] |
| CHO | EC50 |
932 nM
Compound: 1, Endomorphin-1
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Activity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay
Activity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay
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[PMID: 17266203] |
| CHO-K1 | IC50 |
3.2 nM
Compound: 1
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Agonist activity at MOP receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins
Agonist activity at MOP receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins
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[PMID: 23022277] |
| HEK293 | EC50 |
14.4 nM
Compound: 1, EM-1
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Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter
Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter
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[PMID: 22724433] |
| HEK293 | EC50 |
14.4 nM
Compound: EM-1
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Agonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
Agonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
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[PMID: 26403932] |
| HEK293 | EC50 |
61 nM
Compound: EM-1
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Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method
Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method
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[PMID: 32199689] |
| SH-SY5Y | IC50 |
14 nM
Compound: 1, endomorphin 1, endo 1
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Agonist activity at mu opioid receptor in human SHSY5Y cells assessed as inhibition of forskolin-stimulated cAMP production
Agonist activity at mu opioid receptor in human SHSY5Y cells assessed as inhibition of forskolin-stimulated cAMP production
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[PMID: 18468445] |
| SH-SY5Y | IC50 |
65.4 nM
Compound: 1
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Agonist activity at mu-opioid receptor in human SH-SY5Y cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by immunoassay
Agonist activity at mu-opioid receptor in human SH-SY5Y cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by immunoassay
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[PMID: 22680612] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Endomorphin 1 (50 μg/kg, i.v.) alleviates myocardial ischemia/reperfusion injury (MIRI) by inhibiting the inflammatory response[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice[2].
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Dosage:6.16 nM (ED50)
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Administration:Intracerebroventricularly (i.c.v.) injection
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Result:Inhibited dose-dependently the tail-flick response.
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Animal Model:Rats[3].
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Dosage:50 μg/kg
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Administration:Intravenously following LAD ligation for 25 min, subsequently the LAD was reperfused for 120 min.
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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.
Chemical Information
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CAS No. 189388-22-5
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Appearance Solid
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분자량 610.70
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화학식 C34H38N6O5
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Color White to off-white
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Sequence
Tyr-Pro-Trp-Phe-NH2
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Sequence Shortening
YPWF-NH2
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Structure Classification
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Initial Source
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선적
Room temperature in continental US; may vary elsewhere.
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보관
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)
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Commun
Neuropeptide Y neurons mediate opioid-induced itch by disinhibiting GRP-GRPR microcircuits in the spinal cord. [Abstract]2025 Aug 1;16(1):7074. PMID: 40750771 -
Molecules
Identification of Novel PPARγ Partial Agonists Based on Virtual Screening Strategy: In Silico and In Vitro Experimental Validation. [Abstract]2024 Oct 15;29(20):4881. PMID: 39459249 -
용액&용해도
DMSO : ≥ 50 mg/mL (81.87 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (285 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[2]. 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]
[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. [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]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6375 mL | 8.1873 mL | 16.3747 mL | 40.9366 mL |
| 5 mM | 0.3275 mL | 1.6375 mL | 3.2749 mL | 8.1873 mL | |
| 10 mM | 0.1637 mL | 0.8187 mL | 1.6375 mL | 4.0937 mL | |
| 15 mM | 0.1092 mL | 0.5458 mL | 1.0916 mL | 2.7291 mL | |
| 20 mM | 0.0819 mL | 0.4094 mL | 0.8187 mL | 2.0468 mL | |
| 25 mM | 0.0655 mL | 0.3275 mL | 0.6550 mL | 1.6375 mL | |
| 30 mM | 0.0546 mL | 0.2729 mL | 0.5458 mL | 1.3646 mL | |
| 40 mM | 0.0409 mL | 0.2047 mL | 0.4094 mL | 1.0234 mL | |
| 50 mM | 0.0327 mL | 0.1637 mL | 0.3275 mL | 0.8187 mL | |
| 60 mM | 0.0273 mL | 0.1365 mL | 0.2729 mL | 0.6823 mL | |
| 80 mM | 0.0205 mL | 0.1023 mL | 0.2047 mL | 0.5117 mL |
Endomorphin 1 Related Classifications
HY-P0185 Related Classifications
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