[Leu5]-Enkephalin, amide
Based on 1 Customer Validation
[Leu5]-Enkephalin, amide is a δ opioid receptor agonist.
For research use only. We do not sell to patients.
- Purity: 99.76%
- CAS No.: 60117-24-0
- Formula: C28H38N6O6
- Molecular Weight:554.64
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Storage:
Sealed storage, away from moisture and light.
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)
![[Leu5]-Enkephalin, amide Chemical Structure](https://file.medchemexpress.com/product_pic/hy-p1470.gif "Click to View [Leu5]-Enkephalin, amide Chemical Structure")
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All Opioid Receptor Isoforms
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Biological Activity
δ opioid receptor[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SH-SY5Y | IC50 |
26.1 nM
Compound: 6
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Agonist activity at mu opioid receptor assessed as inhibition of forskolin-induced cAMP production in human SH-SY5Y cells pretreated for 24 hrs with DMEM medium after 15 mins
Agonist activity at mu opioid receptor assessed as inhibition of forskolin-induced cAMP production in human SH-SY5Y cells pretreated for 24 hrs with DMEM medium after 15 mins
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[PMID: 18329886] |
| SH-SY5Y | IC50 |
57.8 nM
Compound: 6
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Agonist activity at mu opioid receptor assessed as inhibition of forskolin-induced cAMP production in human SH-SY5Y cells pretreated for 24 hrs with excess ligand after 15 mins
Agonist activity at mu opioid receptor assessed as inhibition of forskolin-induced cAMP production in human SH-SY5Y cells pretreated for 24 hrs with excess ligand after 15 mins
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[PMID: 18329886] |
[Leu5]-Enkephalin causes concentration-dependent, reversible inhibition of pelvic nerve-evoked contractions, with an IC50 value of 2.1 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 60117-24-0
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Appearance Solid
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Molecular Weight 554.64
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Formula C28H38N6O6
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Color White to off-white
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Synonyms
Leu-Enkephalin amide
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Sequence
Tyr-Gly-Gly-Phe-Leu-NH2
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Sequence Shortening
YGGFL-NH2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture and light
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)
Solvent & Solubility
DMSO : 100 mg/mL (180.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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). 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). 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.75 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.75 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Hurley RW, et al. Contribution of endogenous enkephalins to the enhanced analgesic effects of supraspinal mu opioid receptor agonists after inflammatory injury. J Neurosci. 2001 Apr 1;21(7):2536-45. [Content Brief]
[2]. Kennedy C, et al. [Met5]enkephalin acts via delta-opioid receptors to inhibit pelvic nerve-evoked contractions of cat distal colon. Br J Pharmacol. 1987 Oct;92(2):291-8. [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). 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 | 1.8030 mL | 9.0149 mL | 18.0297 mL | 45.0743 mL |
| 5 mM | 0.3606 mL | 1.8030 mL | 3.6059 mL | 9.0149 mL | |
| 10 mM | 0.1803 mL | 0.9015 mL | 1.8030 mL | 4.5074 mL | |
| 15 mM | 0.1202 mL | 0.6010 mL | 1.2020 mL | 3.0050 mL | |
| 20 mM | 0.0901 mL | 0.4507 mL | 0.9015 mL | 2.2537 mL | |
| 25 mM | 0.0721 mL | 0.3606 mL | 0.7212 mL | 1.8030 mL | |
| 30 mM | 0.0601 mL | 0.3005 mL | 0.6010 mL | 1.5025 mL | |
| 40 mM | 0.0451 mL | 0.2254 mL | 0.4507 mL | 1.1269 mL | |
| 50 mM | 0.0361 mL | 0.1803 mL | 0.3606 mL | 0.9015 mL | |
| 60 mM | 0.0300 mL | 0.1502 mL | 0.3005 mL | 0.7512 mL | |
| 80 mM | 0.0225 mL | 0.1127 mL | 0.2254 mL | 0.5634 mL | |
| 100 mM | 0.0180 mL | 0.0901 mL | 0.1803 mL | 0.4507 mL |
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