Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is a peripherally-selective opioid antagonist for the treatment of opioid-induced constipation. Naloxegol oxalate inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract. Chemically, naloxegol is a pegylated (polyethylene glycol-modified) derivative of α-naloxol. Specifically, the 5-α-hydroxyl group of α-naloxol is connected via an ether linkage to the free hydroxyl group of a monomethoxy-terminated n=7 oligomer of PEG.
|Solubility (25°C)||DMSO ≥ 30 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 No authors listed. JAMA. Naloxegol (Movantik) for Opioid-Induced Constipation
 Tejus Anantharamu, et al. J Pharmacol Pharmacother. Naloxegol: First oral peripherally acting mu opioid receptor antagonists for opioid-induced constipation
 Rachel Jones, et al. Am J Hosp Palliat Care. Naloxegol: A Novel Therapy in the Management of Opioid-Induced Constipation
|Related Opioid Receptor Products|
Nalfurafine is an effective and selective agonist of G protein-biased κ-opioid receptor with high translational potential.
Bevenopran (CB-5945) is a peripheral μ-opioid receptor antagonist.
LY2795050 is a short-acting selective κ(kappa)-opioid receptor (KOR) antagonist. LY2795050 has high affinity for the KOR with Ki value of 0.72 nM. LY2795050 can be used for the research of central nervous system dysfunction.
BTRX-335140 is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively. Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats.
GSK1521498 is a novel, potent and selective μ-opioid receptor antagonist.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.