ADL5859 HCl - 10mM in DMSO , CAS No.850173-95-4

CAS: 850173-95-4 Cat. No.: A408564 Peso molecular: 428.96

GRADE & PURITY 10mM in DMSO

Synonyms

Benzamide, N,N-diethyl-4-(5-hydroxyspiro[2H-1-benzopyran-2,4'-piperidin]-4-yl)-, hydrochloride (1:1)

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

ADL5859 HCl is aδ-opioid receptoragonist withKiof 0.8 nM, selectivity against opioid receptor κ, μ, and weak inhibitory activity at the hERG channel. Phase 2.
In vitro

ADL5859 agonizes δ-opioid receptor with a 1000-fold selectivity than µ- or κ-opioid receptor with K_i of 32 nM and 37 nM, respectively.ADL5859 displays weak inhibitory activity at the hERG channel with an IC50 of 78 μM. The EC50 of ADL5859 against δ opioid receptor is 20 nM.

In vivo

At the screening dose of 3 mg/kg p.o., ADL5859 produces 100% reversal of hyperalgesia in the inflamed paw. The oral ED50 of ADL5859 in the FCA mechanical hyperalgesia assay is 1.4 mg/kg. The antihyperalgesia produced by ADL5859 (3 mg/kg, p.o.) is reversed by pretreatment with the δ opioid antagonist naltrindole (0.3 mg/kg s.c.), thus demonstrating a δ receptor mediated effect.In the rat forced swim assay, ADL5859 (3 mg/kg p.o.) produces robust antidepressant-like activity, as evidenced by a significant decrease in the time spent immobile and a significant increase in the time spent swimming. The bioavailability of ADL5859 (3 mg/kg p.o.) in rats and dogs is 33% and 66%, respectively.ADL5859 efficiently reduces inflammatory and neuropathic pain mainly by recruiting δ-opioid receptors expressed by peripheral Nav1.8-expressing neurons.
Cell Data

cell lines：

Concentrations：0 nM-10 nM

Incubation Time：60 minutes

Powder Purity:≥99%

Specifications

Sinónimos

Benzamide, N, N-diethyl-4-(5-hydroxyspiro[2H-1-benzopyran-2, 4'-piperidin]-4-yl)-, hydrochloride (1:1)

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

ADL5859 HCl is a δ-opioid receptor agonist with K_i of 0.8 nM, selectivity against opioid receptor κ, μ, and weak inhibitory activity at the hERG channel. Phase 2.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Tipo de acción

AGONIST

Nombres e identificadores

• Isómeros SMILES: CCN(CC)C(=O)C1=CC=C(C=C1)C2=CC3(CCNCC3)OC4=CC=CC(=C42)O.Cl
• Peso molecular: 428.96
• Reaxy-Rn: 12257215
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12257215&ln=

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 30 mg/mL (72.9 mM); Water: Insoluble; Ethanol: Insoluble