ADL5859 

ADL-5859 is a selective and orally active δ opioid receptor (DOR) agonist with an K_i and an EC₅₀ value of 0.84 and 20 nM, respectively. ADL-5859 also shows inhibitory activity to hERG channel with an IC₅₀ value of 78 μM. ADL-5859 can be used for the research of pain^[1][2].

IC50: 78 μM (hERG channel), 43 μM (CYP2D6)^[1][2]

ADL-5859 (0-10 μM) shows activities to δ opioid receptor with an K_i 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) exhibits inhibitory activity to hERG channel with an IC₅₀ value of 78 μM^[1].
ADL-5859 (0-100 μM) 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.

392.49

C₂₄H₂₈N₂O₃

850305-06-5

O=C(N(CC)CC)C1=CC=C(C2=CC3(CCNCC3)OC4=C2C(O)=CC=C4)C=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. 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), pp 5893-5896

  [2]. 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]

  [3]. 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]