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Product Name: | ADL-5859 hydrochloride | ||||||||||||||||
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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 Ki 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 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) 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].
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