产品
编 号：F478984
分子式：C24H29ClN2O3
分子量：428.95
分子式：C24H29ClN2O3
分子量：428.95
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
50mg
询价
询价
结构图
CAS No: 850173-95-4
产品详情
生物活性：
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.
体内研究：
ADL-5859 (0.3-10 mg/kg; p.o. once) hydrochloride reverses hyperalgesia in inflamed paw of rats and shows robust antidepressant-like activity.1.19Pharmacokinetic Properties of ADL-5859 in Rats and Dogs.RatsIV 0.25 mg/kg and PO 3 mg/kg DogsIV 1 mg/kg and PO 3 mg/kg
CLs (L/h/kg)1.8±0.50.4±0.1
Vdss (L/kg)10.7±1.92.5±0.5
t1/2 (oral, h)5.3±0.74.7±0.2
F (%)33.4±3.266.5±6.8
Animal Model:Rats with Freund’s Complete Adjuvant (FCA) injection induced mechanical hyperalgesia
Dosage:0.3-10 mg/kg
Administration:Oral gavage; 0.3-10 mg/kg once
Result:Produced 100% reversal of hyperalgesia in the inflamed paw with a dose of 3 mg/kg and showed an oral ED50 value of 1.4 mg/kg.
Animal Model:Male Sprague-Dawley rats
Dosage:0.3 and 3 mg/kg
Administration:Oral gavage; 0.3 and 3 mg/kg once
Result:Produced robust antidepressant-like activity in the rat forced swim assay with a dose of 3 mg/kg.
体外研究：
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.
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.
体内研究：
ADL-5859 (0.3-10 mg/kg; p.o. once) hydrochloride reverses hyperalgesia in inflamed paw of rats and shows robust antidepressant-like activity.1.19Pharmacokinetic Properties of ADL-5859 in Rats and Dogs.RatsIV 0.25 mg/kg and PO 3 mg/kg DogsIV 1 mg/kg and PO 3 mg/kg
CLs (L/h/kg)1.8±0.50.4±0.1
Vdss (L/kg)10.7±1.92.5±0.5
t1/2 (oral, h)5.3±0.74.7±0.2
F (%)33.4±3.266.5±6.8
Animal Model:Rats with Freund’s Complete Adjuvant (FCA) injection induced mechanical hyperalgesia
Dosage:0.3-10 mg/kg
Administration:Oral gavage; 0.3-10 mg/kg once
Result:Produced 100% reversal of hyperalgesia in the inflamed paw with a dose of 3 mg/kg and showed an oral ED50 value of 1.4 mg/kg.
Animal Model:Male Sprague-Dawley rats
Dosage:0.3 and 3 mg/kg
Administration:Oral gavage; 0.3 and 3 mg/kg once
Result:Produced robust antidepressant-like activity in the rat forced swim assay with a dose of 3 mg/kg.
体外研究：
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.
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