A peripherally acting antagonist of the μ-opioid receptor (Ki = 7.42 nM; pA2 = 7.95); selective for the μ-opioid receptor over the δ-opioid receptor (Ki = 866 nM); acts as a partial agonist of κ-opioid receptors in vitro (EC50 = 47 nM for [35S]GTPγS binding); reverses morphine-induced decreases in gastrointestinal motility and analgesia in a hot-plate assay in rats (ED50s = 23.1 and 55.4 mg/kg

Naloxegol (oxalate) – 10 mg

Brand:
Cayman
CAS:
1354744-91-4
Storage:
-20
UN-No:
Non-Hazardous - /

Naloxegol is a peripherally acting antagonist of the μ-opioid receptor (Ki = 7.42 nM; pA2 = 7.95).{39588} It is selective for the μ-opioid receptor over the δ-opioid receptor (Ki = 866 nM). Naloxegol also acts as a partial agonist of κ-opioid receptors in vitro (EC50 = 47 nM for [35S]GTPγS binding) but lacks activity ex vivo at concentrations up to 10 μM. In vivo, naloxegol reverses morphine-induced decreases in gastrointestinal motility and analgesia in a hot-plate assay in rats (ED50s = 23.1 and 55.4 mg/kg, respectively), demonstrating a two-fold separation for peripheral versus CNS effects. Naloxegol also exhibits a brain uptake rate comparable to atenolol, a low-permeation standard with no brain uptake, in a rat brain perfusion model.  

 

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SKU: 23731 - 10 mg Category:

Description

A peripherally acting antagonist of the μ-opioid receptor (Ki = 7.42 nM; pA2 = 7.95); selective for the μ-opioid receptor over the δ-opioid receptor (Ki = 866 nM); acts as a partial agonist of κ-opioid receptors in vitro (EC50 = 47 nM for [35S]GTPγS binding); reverses morphine-induced decreases in gastrointestinal motility and analgesia in a hot-plate assay in rats (ED50s = 23.1 and 55.4 mg/kg, respectively); exhibits minimal brain uptake in a rat brain perfusion model

Formal name: (5α,6α)-4,5-epoxy-6-(3,6,9,12,15,18,21-heptaoxadocos-1-yloxy)-17-(2-propen-1-yl)-morphinan-3,14-diol, monoethanedioate

Synonyms:  AZ 13337019|NKTR-118

Molecular weight: 741.8

CAS: 1354744-91-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Pain Research

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