854601-70-0
Chemical Structure
Naloxegol
Synonym(s): NKTR-118; AZ-13337019
- CAS No.: 854601-70-0
- Formula:C34H53NO11
- Molecular Weight:651.78
IUPAC Name: (4R,4aS,7S,7aR,12bS)-7-((2,5,8,11,14,17,20-heptaoxadocosan-22-yl)oxy)-3-allyl-1,2,3,4,5,6,7,7a-octahydro-4aH-4,12-methanobenzofuro[3,2-e]isoquinoline-4a,9-diol
InChIKey: XNKCCCKFOQNXKV-ZRSCBOBOSA-N
SMILES: 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
Biological Activity: Naloxegol (NKTR-118; AZ-13337019) is an orally active peripherally acting μ-opioid receptor antagonist with a target Ki 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].
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Naloxegol | Naloxegol (NKTR-118; AZ-13337019) is an orally active peripherally acting μ-opioid receptor antagonist with a target Ki 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. | |||||||||||||||||||||
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Naloxegol-13C,d2 | Naloxegol-13C,d2 (NKTR-118-13C,d2) is 13C labeled Naloxegol. Naloxegol (NKTR-118; AZ-13337019) is a μ-opioid-receptor antagonist. Naloxegol inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation. | |||||||||||||||||||||
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Naloxegol-13C,d3 | Naloxegol-13C,d3 (NKTR-118-13C,d3) is 13C labeled Naloxegol. Naloxegol (NKTR-118; AZ-13337019) is a μ-opioid-receptor antagonist. Naloxegol inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation. | |||||||||||||||||||||
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References
- [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]
