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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
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 741.82
Formula C36H55NO15
CAS Number 1354744-91-4
Purity >99%
Solubility DMSO ≥ 30 mg/mL
Storage at -20°C
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

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