Naloxegol
Based on 2 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- CAS No.: 854601-70-0
- Formula: C34H53NO11
- Molecular Weight:651.78
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Naloxegol
MoreAll Opioid Receptor Isoforms
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Biological Activity
Description
IC50 & Target
Opioid receptor[1]
In Vitro
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. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 854601-70-0
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Molecular Weight 651.78
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Formula C34H53NO11
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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
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Synonyms
NKTR-118; AZ-13337019
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Front Immunol
Butorphanol Promotes Macrophage Phenotypic Transition to Inhibit Inflammatory Lung Injury via κ Receptors. [Abstract]2021 Jul 7:12:692286. PMID: 34305926 -
Eur J Pharmacol
2021 Jul 15:903:174132. PMID: 33933466
Purity & Documentation
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Naloxegol Related Classifications
HY-A0118 Related Classifications
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