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- 2025年07月13日
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- 保存条件：
4°C, sealed storage, away from moisture
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
850173-95-4
- 规格：
10 mM * 1 mL/5 mg/10 mg/50 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1287.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥1170.0 |
| 规格： | 10 mg | 产品价格： | ￥1980.0 |
| 规格： | 50 mg | 产品价格： | ￥6930.0 |
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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.
1.19
Pharmacokinetic Properties of ADL-5859 in Rats and Dogs.| 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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文献和实验Guanidine Hydrochloride Purification of Proteins From SDS
Pepstatin A (2.0 mg/ml)10 ml Leupeptin (1.0 mg/ml)10 ml Aprotinin (5.0 mg/ml)(Protease Inhibitor Cocktail Sigma #P8340)Denaturation Buffer6 M guanidine hydrochloride 57.3 g G-HCl20 mM Hepes 7.9 2 ml 1M Hepes pH 7.910 mM KCl 0.074 g KCl0.5 mM DTT 100 ml 0.5 M
Guanidine Hydrochloride Purification of Proteins From SDS PAGE
(Sigma #P7626) 10 ml Pepstatin A (2.0 mg/ml) 10 ml Leupeptin (1.0 mg/ml) 10 ml Aprotinin (5.0 mg/ml) (Protease Inhibitor Cocktail Sigma #P8340) Denaturation Buffer 6 M guanidine hydrochloride 57.3 g G-HCl 20 mM Hepes 7.9 2 ml 1M Hepes pH 7.9 10 mM
Packed column subcritical and/or supercritical fluid chromatography (p-sub or pSFC) has been used as a powerful chiral separation technique, whereby a mobile phase produces low viscosity, a high diffusion coefficient, and a solvating power. P
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