Naloxegol-d5 (oxalate)
- CAS No.
- Chemical Name:
- Naloxegol-d5 (oxalate)
- Synonyms
- Naloxegol-d5 (oxalate)
- CBNumber:
- CB56197853
- Molecular Formula:
- Molecular Weight:
- 0
- MDL Number:
- MOL File:
- Mol file
Naloxegol-d5 (oxalate) Chemical Properties, Uses, Production
Description
Naloxegol-d5 is intended for use as an internal standard for the quantification of naloxegol (Item No. 23731) by GC- or LC-MS. 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
[1] EIKE FLOETTMANN. Pharmacologic Profile of Naloxegol, a Peripherally Acting µ-Opioid Receptor Antagonist, for the Treatment of Opioid-Induced Constipation.[J]. Journal of Pharmacology and Experimental Therapeutics, 2017, 361 2: 280-291. DOI: 10.1124/jpet.116.239061
Naloxegol-d5 (oxalate) Preparation Products And Raw materials
Raw materials
Preparation Products
Naloxegol-d5 (oxalate) Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Shanghai Hongye Biotechnology Co. Ltd | 400-9205774 400-920-5774 | sales@glpbio.cn | China | 6705 | 58 |
| ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11123 | 58 |
| TLC Pharmaceutical Standards Ltd. | 18012923235 | chinasales04@tlcstandards.com.cn | China | 8143 | 58 |
| Supplier | Advantage |
|---|---|
| Shanghai Hongye Biotechnology Co. Ltd | 58 |
| ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 58 |
| TLC Pharmaceutical Standards Ltd. | 58 |
