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Naloxegol oxalate

Cat. No. M9784
Naloxegol oxalate Structure
Synonym:

NKTR-118; AZ-13337019 oxalate

Size Price Availability Quantity
10mg USD 90  USD90 In stock
50mg USD 240  USD240 In stock
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Quality Control & Documentation
Biological Activity

Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is a peripherally-selective opioid antagonist for the treatment of opioid-induced constipation. Naloxegol oxalate inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract. Chemically, naloxegol is a pegylated (polyethylene glycol-modified) derivative of α-naloxol. Specifically, the 5-α-hydroxyl group of α-naloxol is connected via an ether linkage to the free hydroxyl group of a monomethoxy-terminated n=7 oligomer of PEG.

Chemical Information
Molecular Weight 741.82
Formula C36H55NO15
CAS Number 1354744-91-4
Solubility (25°C) DMSO ≥ 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] No authors listed. JAMA. Naloxegol (Movantik) for Opioid-Induced Constipation

[2] Tejus Anantharamu, et al. J Pharmacol Pharmacother. Naloxegol: First oral peripherally acting mu opioid receptor antagonists for opioid-induced constipation

[3] Rachel Jones, et al. Am J Hosp Palliat Care. Naloxegol: A Novel Therapy in the Management of Opioid-Induced Constipation

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Keywords: Naloxegol oxalate, NKTR-118; AZ-13337019 oxalate supplier, Opioid Receptor, inhibitors, activators

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