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製品番号: HY-14356

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ADL5859

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

ADL-5859 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 also shows inhibitory activity to hERG channel with an IC₅₀ value of 78 μM. ADL-5859 can be used for the research of pain.

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CAS 番号: 850305-06-5
分子式: C₂₄H₂₈N₂O₃
分子量:392.49

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

ADL5859 構造式

CAS 番号: 850305-06-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

MedChemExpress（MCE）の使用を引用している文献 ADL5859

Eur J Pharmacol. 2016 Jun 15:781:53-9. [Abstract]

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Cell Proliferation/Viability Assay

Cell Proliferation/Viability Assay

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- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
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Publications (1)
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生物活性

製品説明

IC₅₀ & Target

IC50: 78 μM (hERG channel), 43 μM (CYP2D6)^[1]^[2]

Opioid Receptor アイソフォーム固有の製品をすべて表示 :

Cytochrome P450 アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	20 nM Compound: 20, ADL5859	Agonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS binding Agonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS binding	[PMID: 18788723]
HEK293	IC₅₀	78 μM Compound: 20, ADL5859	Inhibition of human ERG channel in HEK293 cells by voltage-clamp method Inhibition of human ERG channel in HEK293 cells by voltage-clamp method	[PMID: 18788723]

体外実験

ADL-5859 (0-10 μM) 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) exhibits inhibitory activity to hERG channel with an IC₅₀ value of 78 μM^[1].
ADL-5859 (0-100 μM) inhibits activity of the drug metabolizing enzyme cytochrome P450 2D6 (CYP2D6) in vitro with an IC₅₀ value of 43 μM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

化学情報

CAS 番号 850305-06-5
分子量 392.49
分子式 C₂₄H₂₈N₂O₃
SMILES

O=C(N(CC)CC)C1=CC=C(C2=CC3(CCNCC3)OC4=C2C(O)=CC=C4)C=C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (1)

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Eur J Pharmacol

Synergistic antidepressant-like effects between a kappa opioid antagonist (LY2444296) and a delta opioid agonist (ADL5859) in the mouse forced swim test. [Abstract]

2016 Jun 15:781:53-9. PMID: 27044434

ADL5859 purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2016 Jun 15:781:53-9. [Abstract]

The DOR agonist ADL5859 shows antidepressant-like effects in the FST in C57BL/6J mice.

純度とドキュメンテーション

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純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (272 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Potent, Orally Bioavailable Delta Opioid Receptor Agonists for the Treatment of Pain: Discovery of N,N-Diethyl-4-(5-hydroxyspiro[chromene-2,4′-piperidine]-4-yl)benzamide (ADL5859) J. Med. Chem., 2008, 51 (19), pp 5893-5896

[2]. Le Bourdonnec B, et al. Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859). J Med Chem. 2008 Oct 9;51(19):5893-6. [Content Brief]

[3]. Le Bourdonnec B, et al. Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) benzamide (ADL5747).J Med Chem. 2009 Sep 24;52(18):5685-702. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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ADL5859

1 Cited Publications

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生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
化学情報
Publications (1)
純度とドキュメンテーション
参考文献

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ADL5859 purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2016 Jun 15:781:53-9. [Abstract]

Customer Validation
The DOR agonist ADL5859 shows antidepressant-like effects in the FST in C57BL/6J mice.

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ADL5859

MedChemExpress（MCE）の使用を引用している文献 ADL5859

Opioid Receptor アイソフォーム固有の製品をすべて表示

Cytochrome P450 アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (1)

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

ADL5859 関連分類

HY-14356 関連分類