ADL-5859

CAS: 850173-95-4 F: C24H29ClN2O3 W: 428.95

ADL-5859 (compound 20) is a selective and orally active δ opioid receptor (DOR) agonist with an Ki and an EC50 value of

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Bioactivity	ADL-5859 (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 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].
Target	IC50: 78 μM (hERG channel), 43 μM (CYP2D6)
Invitro	ADL-5859 (0-10 μM) 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) 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].
In Vivo	ADL-5859 (0.3-10 mg/kg; p.o. once) reverses hyperalgesia in inflamed paw of rats and shows robust antidepressant-like activity[1].1.19Pharmacokinetic Properties of ADL-5859 in Rats and Dogs[1].
Name	ADL-5859
CAS	850173-95-4
Formula	C24H29ClN2O3
Molar Mass	428.95
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[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. [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.