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ADL-5859 hydrochloride Data Sheet

Product Name:

ADL-5859 hydrochloride

CAS No.:

850173-95-4

Cat. No.:

HY-13044

MWt:

428.95

Formula:

C24H29ClN2O3

Purity :

>98%

Solubility:

DMSO : ≥ 100 mg/mL;H<sub>2</sub>O : 5 mg/mL (ultrasonic;warming;heat to 60°C)

Mechanisms:

Target: Inflammation/Immunology Neurological Disease

Biological Activity:

ADL-5859 hydrochloride (compound 20) 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 hydrochloride also shows inhibitory activity to hERG channel with an IC₅₀ value of 78 μM. ADL-5859 hydrochloride can be used for the research of pain^[1]^[2]. IC50 & Target:IC50: 78 μM (hERG channel), 43 μM (CYP2D6)^[1]^[2] In Vitro:ADL-5859 (0-10 μM) hydrochloride 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) hydrochloride exhibits inhibitory activity to hERG channel with an IC₅₀ value of 78 μM^[1].
ADL-5859 (0-100 μM) hydrochloride 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) hydrochloride reverses hyperalgesia in inflamed paw of rats and shows robust antidepressant-like activity^[1].
1.19 Pharmacokinetic Properties of ADL-5859 in Rats and Dogs^[1].

	Rats IV 0.25 mg/kg and PO 3 mg/kg	Dogs IV 1 mg/kg and PO 3 mg/kg
CLs (L/h/kg)	1.8±0.5	0.4±0.1
Vdss (L/kg)	10.7±1.9	2.5±0.5
t_1/2 (oral, h)	5.3±0.7	4.7±0.2
F (%)	33.4±3.2	66.5±6.8

Caution: Not fully tested. For research purposes only

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