ADL5859 HCL
ADL5859 HCl
CAS: 850173-95-4
Molecular Formula: C24H29ClN2O3
ADL5859 HCL - Names and Identifiers
ADL5859 HCL - Physico-chemical Properties
| Molecular Formula | C24H29ClN2O3 |
| Molar Mass | 428.95166 |
| Storage Condition | -20℃ |
| In vitro study | ADL5859 independently stimulated δ-opioid receptors with 1000-fold higher specificity than μ-or κ-opioid receptors under 32nm and 37NM Ki conditions. Under 78um IC50 conditions, ADL5859 showed a weak inhibitory effect on the hERG channel. The EC50 value of ADL5859 for the δ-opioid receptor is 20nm. ADL5859 independently stimulated δ-opioid receptors with 1000-fold higher specificity than μ-or κ-opioid receptors at 32nm and 37NM K I. Under 78um IC50 conditions, ADL5859 showed a weak inhibitory effect on the hERG channel. The EC50 value of ADL5859 for the δ-opioid receptor is 20nm. |
| In vivo study | Under the screening condition of 3 mg/kg orally, ADL5859 can cause 100% reversal of hyperalgesia in the inflamed paw test. The ED50 value of ADL5859 for the oral test in the FCA hyperalgesia mechanism experiment was 1.4 mg/kg. The anti-hyperalgesic phenomenon caused by ADL5859 can be reversed by pretreatment with a delta-opioid receptor antagonist (0.3 mg/kg subcutaneously injected with naltrexole), thus, it was demonstrated that δ-opioid receptors are involved in the mediated response. ADL5859(3 mg/kg P. O.) produced a strong antidepressant-like effect in the forced swimming test in rats, with a significant decrease in pause time and a significant increase in swimming time seen in rats. The bioavailability of ADL5859(3 mg/kg P. O.) was 33% in rats and 66% in dogs. ADL5859 is highly effective in reducing inflammatory responses and neuropathic pain by recruiting δ-opioid receptors expressed by peripheral nav1.8-expressing neurons. Under the screening condition of oral administration at 3 mg/kg, ADL5859 caused 100% reversal of hyperalgesia in the inflamed paw test. The ED50 value of ADL5859 for the oral test in the FCA hyperalgesia mechanism experiment was 1.4 mg/kg. The anti-hyperalgesic phenomenon caused by ADL5859 can be reversed by pretreatment with a delta-opioid receptor antagonist (0.3 mg/kg subcutaneously injected with naltrexole), thus, it was demonstrated that δ-opioid receptors are involved in the mediated response. ADL5859(3 mg/kg P. O.) produced a strong antidepressant-like effect in the forced swimming test in rats, with a significant decrease in pause time and a significant increase in swimming time seen in rats. The bioavailability of ADL5859(3 mg/kg P. O.) was 33% in rats and 66% in dogs. ADL5859 is highly effective in reducing inflammatory responses and neuropathic pain by recruiting δ-opioid receptors expressed by peripheral nav1.8-expressing neurons. |
ADL5859 HCL - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.331 ml | 11.656 ml | 23.312 ml |
| 5 mM | 0.466 ml | 2.331 ml | 4.662 ml |
| 10 mM | 0.233 ml | 1.166 ml | 2.331 ml |
| 5 mM | 0.047 ml | 0.233 ml | 0.466 ml |
Last Update：2024-01-02 23:10:35
ADL5859 HCL - Introduction
Nature:
ADL5859 HCl is a white solid powder that can be dissolved in water. Its chemical structure contains phenyl, oxygen atom, 3-fluorine and 1H-Tetrazole group.
Use:
ADL5859 HCl is a specific κ-opioid receptor agonist that selectively activates κ-opioid receptors. This compound is often used in scientific research to study the mechanism of action of the κ-opioid receptor, signaling pathways, and potential drug candidates.
Preparation Method:
The preparation method of ADL5859 HCl is mainly obtained by chemical synthesis. General preparation procedures involve processes such as reaction, crystallization, and purification of appropriate starting materials.
Safety Information:
ADL5859 HCl is a laboratory compound that requires compliance with relevant safety procedures. It may be irritating and dangerous to the human body, so it is necessary to wear appropriate protective equipment during use, such as laboratory gloves, glasses and laboratory clothing. In addition, it should be stored in a dry, dark and sealed container, away from ignition and flammable materials.
Please note that ADL5859 HCl is a professional laboratory compound for scientific purposes only. When using, please follow the relevant regulations and safety procedures to ensure safety.
Last Update：2024-04-09 20:52:54
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CAS: 850173-95-4
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CAS: 850173-95-4
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