Naloxegol oxalate
Based on 2 publication(s) in Google Scholar
Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is an orally active peripherally acting μ-opioid receptor antagonist with a target Ki of 7.42 nM. Naloxegol oxalate 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 oxalate is applicable to research related to opioid-induced constipation.
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- Pureté: 99.91%
- CAS No.: 1354744-91-4
- Formule: C36H55NO15
- Masse moléculaire:741.82
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Naloxegol oxalate
MoreVoir tous les produits spécifiques à Isoform Opioid Receptor
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Activité biologique
Opioid receptor[1]
Naloxegol oxalate 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1354744-91-4
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Appearance Solid
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Masse moléculaire 741.82
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Formule C36H55NO15
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Color White to off-white
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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.OC(C(O)=O)=O
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Synonyms
NKTR-118 oxalate; AZ-13337019 oxalate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
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
Solvant et solubilité
H2O : ≥ 100 mg/mL (134.80 mM)
DMSO : 50 mg/mL (67.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (2.80 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (2.80 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureté et documentation
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Fiche technique (271 KB)
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SDS (644 KB)
- English - EN (644 KB)
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Instruction de manipulation (2659 KB)
Références
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 1.3480 mL | 6.7402 mL | 13.4804 mL | 33.7009 mL |
| 5 mM | 0.2696 mL | 1.3480 mL | 2.6961 mL | 6.7402 mL | |
| 10 mM | 0.1348 mL | 0.6740 mL | 1.3480 mL | 3.3701 mL | |
| 15 mM | 0.0899 mL | 0.4493 mL | 0.8987 mL | 2.2467 mL | |
| 20 mM | 0.0674 mL | 0.3370 mL | 0.6740 mL | 1.6850 mL | |
| 25 mM | 0.0539 mL | 0.2696 mL | 0.5392 mL | 1.3480 mL | |
| 30 mM | 0.0449 mL | 0.2247 mL | 0.4493 mL | 1.1234 mL | |
| 40 mM | 0.0337 mL | 0.1685 mL | 0.3370 mL | 0.8425 mL | |
| 50 mM | 0.0270 mL | 0.1348 mL | 0.2696 mL | 0.6740 mL | |
| 60 mM | 0.0225 mL | 0.1123 mL | 0.2247 mL | 0.5617 mL | |
| H2O | 80 mM | 0.0169 mL | 0.0843 mL | 0.1685 mL | 0.4213 mL |
| 100 mM | 0.0135 mL | 0.0674 mL | 0.1348 mL | 0.3370 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Naloxegol oxalate Related Classifications
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