ADL-5859 hydrochloride
Based on 1 publication(s) in Google Scholar
ADL-5859 hydrochloride (compound 20) is a selective and orally active δ opioid receptor (DOR) agonist with an Ki and an EC50 value of 0.84 and 20 nM, respectively. ADL-5859 hydrochloride also shows inhibitory activity to hERG channel with an IC50 value of 78 μM. ADL-5859 hydrochloride can be used for the research of pain.
For research use only. We do not sell to patients.
- Purity: 98.96%
- CAS No.: 850173-95-4
- Formula: C24H29ClN2O3
- Molecular Weight:428.95
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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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Publications Citing Use of MedChemExpress (MCE) ADL-5859 hydrochloride
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Customer Validation & Images
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Cell Proliferation/Viability Assay
All Opioid Receptor Isoforms
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Biological Activity
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δ Opioid Receptor/DOR |
ADL-5859 (0-10 μM) hydrochloride shows activities to δ opioid receptor with an Ki and an EC50 value of 0.84 and 20 nM, and inhibits 32% and 37% activities to μ and κ opioid receptor, respectively[1]. ADL-5859 (0-100 μM) hydrochloride exhibits inhibitory activity to hERG channel with an IC50 value of 78 μM[1]. ADL-5859 (0-100 μM) hydrochloride inhibits activity of the drug metabolizing enzyme cytochrome P450 2D6 (CYP2D6) in vitro with an IC50 value of 43 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Rats IV 0.25 mg/kg and PO 3 mg/kg |
Dogs IV 1 mg/kg and PO 3 mg/kg |
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| CLs (L/h/kg) | 1.8±0.5 | 0.4±0.1 |
| Vdss (L/kg) | 10.7±1.9 | 2.5±0.5 |
| t1/2 (oral, h) | 5.3±0.7 | 4.7±0.2 |
| F (%) | 33.4±3.2 | 66.5±6.8 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats with Freund’s Complete Adjuvant (FCA) injection induced mechanical hyperalgesia[1]
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Dosage:0.3-10 mg/kg
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Administration:Oral gavage; 0.3-10 mg/kg once
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Result:Produced 100% reversal of hyperalgesia in the inflamed paw with a dose of 3 mg/kg and showed an oral ED50 value of 1.4 mg/kg.
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Animal Model:Male Sprague-Dawley rats[1]
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Dosage:0.3 and 3 mg/kg
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Administration:Oral gavage; 0.3 and 3 mg/kg once
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Result:Produced robust antidepressant-like activity in the rat forced swim assay with a dose of 3 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 850173-95-4
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Appearance Solid
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Molecular Weight 428.95
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Formula C24H29ClN2O3
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Color White to off-white
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SMILES
OC1=C2C(OC3(C=C2C4=CC=C(C=C4)C(N(CC)CC)=O)CCNCC3)=CC=C1.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Eur J Pharmacol
Synergistic antidepressant-like effects between a kappa opioid antagonist (LY2444296) and a delta opioid agonist (ADL5859) in the mouse forced swim test. [Abstract]2016 Jun 15:781:53-9. PMID: 27044434
ADL-5859 hydrochloride purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2016 Jun 15:781:53-9. [Abstract]
The DOR agonist ADL5859 shows antidepressant-like effects in the FST in C57BL/6J mice.
Solvent & Solubility
DMSO : ≥ 100 mg/mL (233.13 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 5 mg/mL (11.66 mM; ultrasonic and warming and heat to 60°C)
* "≥" 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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: ≥ 2.75 mg/mL (6.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: ≥ 2.75 mg/mL (6.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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)
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 (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Le Bourdonnec B, et al. Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859). J Med Chem. 2008 Oct 9;51(19):5893-6. [Content Brief]
[2]. Le Bourdonnec B, et al. Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) benzamide (ADL5747).J Med Chem. 2009 Sep 24;52(18):5685-702. [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). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.3313 mL | 11.6564 mL | 23.3127 mL | 58.2818 mL |
| 5 mM | 0.4663 mL | 2.3313 mL | 4.6625 mL | 11.6564 mL | |
| 10 mM | 0.2331 mL | 1.1656 mL | 2.3313 mL | 5.8282 mL | |
| DMSO | 15 mM | 0.1554 mL | 0.7771 mL | 1.5542 mL | 3.8855 mL |
| 20 mM | 0.1166 mL | 0.5828 mL | 1.1656 mL | 2.9141 mL | |
| 25 mM | 0.0933 mL | 0.4663 mL | 0.9325 mL | 2.3313 mL | |
| 30 mM | 0.0777 mL | 0.3885 mL | 0.7771 mL | 1.9427 mL | |
| 40 mM | 0.0583 mL | 0.2914 mL | 0.5828 mL | 1.4570 mL | |
| 50 mM | 0.0466 mL | 0.2331 mL | 0.4663 mL | 1.1656 mL | |
| 60 mM | 0.0389 mL | 0.1943 mL | 0.3885 mL | 0.9714 mL | |
| 80 mM | 0.0291 mL | 0.1457 mL | 0.2914 mL | 0.7285 mL | |
| 100 mM | 0.0233 mL | 0.1166 mL | 0.2331 mL | 0.5828 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
ADL-5859 hydrochloride Related Classifications
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