SKU: A172  / 
    CAS Number: 156053-89-3

    Alvimopan

    $89.25 - $845.25

    Alvimopan is a gastroprokinetic peripherally restricted mu-opioid receptor antagonist (MOR). It has a favorable kinetic activity (0.2 ng/ml) and dissociates more slowly than most other ligands.

    Mechanism of ActionAlvimopan competitively binds to the mu-opioid receptor in the gastrointestinal tract. It has a low systemic absorption and a high affinity for mu-opioid receptors. This compound assists gastrointestinal motility dysfunction.
    Purity Level98.0%-102.0% (anhydrous basis)02.0% (anhydrous basis)
    Eukaryotic Cell Culture ApplicationsIn vitro studies with Alvimopan using CHO cell membranes revealed that it inhibited GTP binding with an IC50 of 1.7 nM.
    Molecular FormulaC25H32N2O4
    SolubilitySlightly soluble in DMSO. Very slightly soluble in water.
    ReferencesBeattie DT (2007) The in vitro pharmacology of the peripherally restricted opioid receptor antagonists, Alvimopan, ADL 08-0011 and methylnaltrexone. Naunyn Schmiedebergs Arch Pharmacol. 375(3):205-220 PMID 17340127 Cassel JA, Daubert JD and DeHaven RN (2005) [(3)H] Alvimopan binding to the micro opioid receptor: comparative binding kinetics of opioid antagonists. Eur. J. Pharmacol 520(1-3):29-36 PMID 16165125 Camilleri M (2005) Alvimopan, a selective peripherally acting µ-opioid antagonist. Neurogastroenterol. & Motil. 172):157-165 Fukuda H (2006) The selective mu opioid receptor antagonist, Alvimopan, improves delayed GI transit of postoperative ileus in rats. Brain Res.102(1):63-70 PMID 16797494 Kaserer T et al (2016) μ Opioid receptor: novel antagonists and structural modeling. Sci. Rep 6:21548 PMID 26888328 Schmidt WK (2001) Alvimopan (ADL 8-2698) is a novel peripherla opioid antagonist. A. J. Surg. 182(5):S27-S38