ADL-5859 hydrochloride | MedChemExpress (MCE)
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MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。ADL-5859 hydrochlorideCAS No. : 850173-95-4MCE 国际站：ADL-5859 hydrochloride产品活性：ADL
MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。
ADL-5859 hydrochloride
CAS No. : 850173-95-4
MCE 国际站：ADL-5859 hydrochloride
产品活性：ADL-5859 hydrochloride (compound 20) 是选择性的、具有口服活性的 δ opioid receptor (DOR) 激动剂，Ki 值为 0.84 nM，EC50 值为 20 nM。ADL-5859 hydrochloride 对 hERG 具有抑制活性，IC50 值为 78 μM。ADL-5859 hydrochloride 可用于痛觉的研究。
研究领域：GPCR/G Protein | Neuronal Signaling | Membrane Transporter/Ion Channel | Metabolic Enzyme/Protease
作用靶点：Opioid Receptor | Potassium Channel | Cytochrome P450
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.ADL-5859 (0-100 μM) hydrochloride exhibits inhibitory activity to hERG channel with an IC50 value of 78 μM.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.
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.
| 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 |
| t1/2 (oral, h) | 5.3±0.7 | 4.7±0.2 |
| F (%) | 33.4±3.2 | 66.5±6.8 |
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