Naloxegol-d5 (oxalate)

Formulation: A solid

Formal Name: (4R,4aS,7S,7aR,12bS)-7-((2,5,8,11,14,17,20-heptaoxadocosan-22-yl)oxy)-3-(allyl-d5)-1,2,3,4,5,6,7,7a-octahydro-4aH-4,12-methanobenzofuro[3,2-e]isoquinoline-4a,9-diol, monoethanedioate

Purity: ≥99% deuterated forms (d1-d5)

Formula Markup: C34H48D5NO11 • C2H2O4

Formula Weight: 746,9

Shelf life (days): 1460

Notes: Naloxegol-d5 is intended for use as an internal standard for the quantification of naloxegol (Item No. 23731) by GC- or LC-MS. 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.

• Artikelnummer: CAY29578
• Hersteller: Cayman Chemical
• Hersteller Artikelnummer: 29578-1
• Green Labware: Nein
• Verpackungseinheit: 1 mg
• Mengeneinheit: STK
• Methode: GC-MS, LC-MS, Isotopenmarkierung