A peripherally acting antagonist of the μ-opioid receptor
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Labeled Version(s)
29578Naloxegol-d5 (oxalate)
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Naloxegol (oxalate)

Item No. 23731

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(5α,6α)-4,5-epoxy-6-(3,6,9,12,15,18,21-heptaoxadocos-1-yloxy)-17-(2-propen-1-yl)-morphinan-3,14-diol, monoethanedioate
CAS Number
1354744-91-4
Synonyms
  • AZ 13337019
  • NKTR-118
Molecular Formula
C34H53NO11 • C2H2O4
Formula Weight
741.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMSO: 20 mg/mlEthanol: 30 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
212 nm
SMILES
O[C@]12[C@]3(CCN(CC=C)[C@@H]2C4)[C@](OC5=C3C4=CC=C5O)([H])[C@@H](OCCOCCOCCOCCOCCOCCOCCOC)CC1.OC(C(O)=O)=O
InChi Code
InChI=1S/C34H53NO11.C2H2O4/c1-3-9-35-10-8-33-30-26-4-5-27(36)31(30)46-32(33)28(6-7-34(33,37)29(35)25-26)45-24-23-44-22-21-43-20-19-42-18-17-41-16-15-40-14-13-39-12-11-38-2;3-1(4)2(5)6/h3-5,28-29,32,36-37H,1,6-25H2,2H3;(H,3,4)(H,5,6)/t28-,29+,32-,33-,34+;/m0./s1
InChi Key
MNYIRXLCPODKLG-VUTNLTPYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $196

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    10 mg

    $351

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    25 mg

    $631

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    50 mg

    $1,029

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    Product Description

    Naloxegol is a peripherally acting antagonist of the μ-opioid receptor (Ki = 7.42 nM; pA2 = 7.95).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Floettmann, E., Bui, K., Sostek, M., et al. Pharmacologic profile of naloxegol, a peripherally acting µ-opioid receptor antagonist, for the treatment of opioid-induced constipation. J. Pharmacol. Exp. Ther. 361(2), 280-291 (2017).