Naloxegol  (Synonyms: NKTR-118; AZ-13337019)

Naloxegol (NKTR-118; AZ-13337019) is an orally active peripherally acting μ-opioid receptor antagonist with a target K_i of 7.42 nM. Naloxegol inhibits the binding of opioids to μ-opioid receptors in the gastrointestinal tract, and alleviates opioid-induced gastrointestinal hypomotility, delayed transit, hypertonicity, and increased fluid reabsorption. Naloxegol is applicable to research related to opioid-induced constipation^[1][2].

Opioid receptor^[1]

Naloxegol binds with high affinity to μ-opioid receptors and κ-opioid receptors and low affinity to δ-opioid receptors in vitro, with no significant activity at non-opioid targets^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Naloxegol inhibits the binding of opioids to μ-opioid receptors in the gastrointestinal tract, and alleviates the opioid-induced phenomena including slowed gastrointestinal motility and transit, hypertonicity, and increased fluid reabsorption^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

651.78

C₃₄H₅₃NO₁₁

854601-70-0

O[C@@]1(CC[C@H](OCCOCCOCCOCCOCCOCCOCCOC)[C@]2([H])OC3=C4O)[C@]52C3=C(C=C4)C[C@@]1([H])N(CC=C)CC5

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Corsetti M, et al. Naloxegol: the first orally administered, peripherally acting, mu opioid receptor antagonist, approved for the treatment of opioid-induced constipation. Drugs Today (Barc). 2015;51(8):479-489.  [Content Brief]

  [2]. Garnock-Jones KP, et al. Naloxegol: a review of its use in patients with opioid-induced constipation. Drugs. 2015;75(4):419-425.  [Content Brief]