ADL5859 HCl

Catalog No.S1139

ADL5859 HCl Chemical Structure

Molecular Weight(MW): 428.95

ADL5859 HCl is a δ-opioid receptor agonist with Ki of 0.8 nM, selectivity against opioid receptor κ, μ, and weak inhibitory activity at the hERG channel. Phase 2.

Size Price Stock Quantity  
In DMSO USD 290 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
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1 Customer Review

  • ADL-5859 respectively ADL-5747 were dopioid agonists (DORs) which were developed as analgesics for post-operative, neuropathic or musculoskeletal pain. They were expected to have superior analgesic potency over the existing ones, due to the different receptor targeted. However their development was stopped due to unconvincing efficacy.

    University of Hong Kong. ADL5859 HCl purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description ADL5859 HCl is a δ-opioid receptor agonist with Ki of 0.8 nM, selectivity against opioid receptor κ, μ, and weak inhibitory activity at the hERG channel. Phase 2.
Targets
δ-opioid receptor [1] μ-opioid receptor [1] κ-opioid receptor [1]
0.8 nM(Ki) 32 nM(Ki) 37 nM(Ki)
In vitro

ADL5859 agonizes δ-opioid receptor with a 1000-fold selectivity than µ- or κ-opioid receptor with Ki of 32 nM and 37 nM, respectively.ADL5859 displays weak inhibitory activity at the hERG channel with an IC50 of 78 μM. The EC50 of ADL5859 against δ opioid receptor is 20 nM.[1]

In vivo At the screening dose of 3 mg/kg p.o., ADL5859 produces 100% reversal of hyperalgesia in the inflamed paw. The oral ED50 of ADL5859 in the FCA mechanical hyperalgesia assay is 1.4 mg/kg. The antihyperalgesia produced by ADL5859 (3 mg/kg, p.o.) is reversed by pretreatment with the δ opioid antagonist naltrindole (0.3 mg/kg s.c.), thus demonstrating a δ receptor mediated effect.In the rat forced swim assay, ADL5859 (3 mg/kg p.o.) produces robust antidepressant-like activity, as evidenced by a significant decrease in the time spent immobile and a significant increase in the time spent swimming. The bioavailability of ADL5859 (3 mg/kg p.o.) in rats and dogs is 33% and 66%, respectively.[1]ADL5859 efficiently reduces inflammatory and neuropathic pain mainly by recruiting δ-opioid receptors expressed by peripheral Nav1.8-expressing neurons.[2]

Protocol

Cell Research:[1]
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  • Cell lines: Chinese hamster ovary (CHO) cells stably expressing human κ, μ, or δ opioid receptors
  • Concentrations: 0 nM-10 nM
  • Incubation Time: 60 minutes
  • Method: Membrane preparations from Chinese hamster ovary (CHO) cells stably expressing human κ, μ, or δ opioid receptors are prepared. The assay buffer used is composed of 50 mMtris(hydroxymethyl) aminomethaneHCl, pH 7.8, 1.0 mM ethylene glycol bis(β-aminoethyl ether)-N,N,N',N'-tetraacetic acid (EGTA free acid), 5.0 mM MgCl2 10 mg/L leupeptin, 10 mg/L pepstatin A, 200 mg/L bacitracin, and 0.5 mg/L aprotinin. After dilution in assay buffer and homogenization in a Polytron homogenizer for 30 seconds, membrane proteins (10-80 μg) in 250 μL of assay buffer are added to mixtures containing ADL5859 and [3H]diprenorphine (0.5-1.0 nM, 25000-50000 dpm) in 250 μL of assay buffer in 96-well deep-well polystyrene titer plates and incubated at room temperature for 60 minutes. Reactions are terminated by vacuum filtration with a Brandel MPXR-96T harvester through GF/B filters that have been pretreated with a solution of 0.5% polyethylenimine and 0.1% bovine serum albumin for at least 1 hour. The filters arewashed four times with 1.0 mL each of ice-cold 50 mM Tris-HCl, pH 7.8, and 30 μL of Microscint-20 is added to each filter. Radioactivity on the filters is determined by scintillation spectrometry in a Packard TopCount. [3H]Diprenorphine with a specific activity of 50 Ci/mmolisused. The Kd values for [3H]diprenorphine binding are 0.33 nM for the κ and μ receptors and 0.26 nM for the δ receptor. Receptor expression levels, determined as Bmax values from Scatchard analyses, are 4400, 4700, and 2100 fmol/mg of protein for the κ, μ, and δ receptors, respectively. Preliminary experiments are performed to show that no specific binding is lost during the wash of the filters, that binding achieved equilibrium within the incubation time and remained at equilibrium for at least an additional 60 minutes, and that binding is linear with regard to protein concentration. Nonspecific binding, determined in the presence of 10 μM unlabeled naloxone, is less than 10% of total binding. Protein is quantified by the method of Bradford. The data from competition experiments are fit by nonlinear regression analysis with the program Prism using the four-parameter equation for one-site competition, and Ki values are subsequently calculated from EC50 values by the Cheng-Prusoff equation.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: Nav1.8-cKO mice, CMV-KO mice, C57BL6/J × SV129Pas mice
  • Formulation: 0.5% hydroxypropyl methylcellulose/0.1% Tween 80
  • Dosages: 10 mg/kg - 300 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 86 mg/mL (200.48 mM)
Water 5 mg/mL (11.65 mM)
Ethanol 1 mg/mL (2.33 mM)
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% hydroxyethyl cellulose+0.1% Tween 80
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 428.95
Formula

C24H28N2O3.HCl

CAS No. 850173-95-4
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00979953 Completed Osteoarthritis of the Knee Cubist Pharmaceuticals LLC|Pfizer October 2009 Phase 2
NCT00603265 Completed Peripheral Neuropathy|Neuropathic Pain Cubist Pharmaceuticals LLC November 2007 Phase 2
NCT00626275 Completed Rheumatoid Arthritis Cubist Pharmaceuticals LLC October 2007 Phase 2
NCT00993863 Completed Acute Pain Cubist Pharmaceuticals LLC June 2007 Phase 2

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Opioid Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID