ADL5859 HClδ-opioid receptor agonist,selective CAS# 850173-95-4 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 850173-95-4 | SDF | Download SDF |
| PubChem ID | 46931003 | Appearance | Powder |
| Formula | C24H29ClN2O3 | M.Wt | 428.95 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 100 mg/mL (233.13 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide;hydrochloride | ||
| SMILES | CCN(CC)C(=O)C1=CC=C(C=C1)C2=CC3(CCNCC3)OC4=C2C(=CC=C4)O.Cl | ||
| Standard InChIKey | ZFNLSWREIULTDO-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C24H28N2O3.ClH/c1-3-26(4-2)23(28)18-10-8-17(9-11-18)19-16-24(12-14-25-15-13-24)29-21-7-5-6-20(27)22(19)21;/h5-11,16,25,27H,3-4,12-15H2,1-2H3;1H | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | ADL5859 HCl is a selective agonist of δ-opioid receptor with Ki value of 0.84 nM. | |||||
| Targets | δ-opioid receptor | |||||
| IC50 | 0.84 nM (Ki) | |||||
ADL5859 HCl Dilution Calculator
ADL5859 HCl Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.3313 mL | 11.6564 mL | 23.3127 mL | 46.6255 mL | 58.2819 mL |
| 5 mM | 0.4663 mL | 2.3313 mL | 4.6625 mL | 9.3251 mL | 11.6564 mL |
| 10 mM | 0.2331 mL | 1.1656 mL | 2.3313 mL | 4.6625 mL | 5.8282 mL |
| 50 mM | 0.0466 mL | 0.2331 mL | 0.4663 mL | 0.9325 mL | 1.1656 mL |
| 100 mM | 0.0233 mL | 0.1166 mL | 0.2331 mL | 0.4663 mL | 0.5828 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Selective δ opioid receptor agonists are promising potential therapeutic agents for the treatment of various types of pain conditions. A spirocyclic derivative was identified as a promising hit through screening. ADL5859 is a potent, selective, and orally bioavailable δ opioid receptor agonist.
In vitro: ADL5859 displayed subnanomolar binding affinity at the δ opioid receptor, potent δ agonist activity, and excellent opioid receptor selectivity. Moreover, ADL5859 showed weak inhibitory activity at the hERG channel (78 μM) [1].
In vivo: On the basis of its favorable profile in vitro, ADL5859 was tested in the rat Freund’s complete adjuvant (FCA) mechanical hyperalgesia assay. At the screening dose of 3 mg/kg po, ADL5859 produced 100% reversal of hyperalgesia in the inflamed paw. The oral ED50 of ADL5859 in the FCA mechanical hyperalgesia assay was 1.4 mg/kg. The antihyperalgesia produced by ADL5859 (3 mg/kg, po) was reversed by pretreatment with the δ opioid antagonist naltrindole (0.3 mg/kg sc), thus demonstrating a δ receptor mediated effect. Therefore, ADL5859 was selected as a clinical candidate for the treatment of pain [1].
Clinical trial: A clinical study has been conducted to investigate the efficacy and safety of ADL5859 and ADL5747 in participants with pain due to osteoarthritis of the knee, which was supposed to be finished in the middle of 2015.
Reference:
[1] Le Bourdonnec B, Windh RT, Ajello CW, Leister LK, Gu M, Chu GH, Tuthill PA, Barker WM, Koblish M, Wiant DD, Graczyk TM, Belanger S, Cassel JA, Feschenko MS, Brogdon BL, Smith SA, Christ DD, Derelanko MJ, Kutz S, Little PJ, DeHaven RN, DeHaven-Hudkins DL, Dolle RE. 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;51(19):5893-6.
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