Naloxegol


Catalog No. size PriceQuantity
M6640-C CUSTOMER ORDER $9,996

Description

Cas:854601-70-0 (free base)

     1354744-91-4 (oxalate)

Product Information

Naloxegol, also known as and NKTR-118 and AZ-13337019, is a peripherally-selective opioid antagonist for the treatment of opioid-induced constipation. It was approved in 2014 in adult patients with chronic, non-cancer pain. 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 Formula: C36H55NO15

 

Molecular Weight: 741.828

 

Elemental Analysis: C, 58.29; H, 7.47; N, 1.89; O, 32.35

 

Synonym: 

 

NKTR-118

NKTR 118

NKTR118

AZ-13337019

AZ13337019

AZ 13337019

EGylated naloxol

Naloxegol Oxalate

trade names Movantik and Moventig

 

Chemical Name:

(4R,4aS,7S,7aR,12bS)-7-((2,5,8,11,14,17,20-heptaoxadocosan-22-yl)oxy)-3-allyl-1,2,3,4,5,6,7,7a-octahydro-4aH-4,12-methanobenzofuro[3,2-e]isoquinoline-4a,9-diol oxalate

 

InChi Key:

MNYIRXLCPODKLG-VUTNLTPYSA-N

 

InChi Code:

InChI=1S/C34H53NO11.C2H2O4/c1-3-9-35-10-8-33-30-26-4-5-27(36)31(30)46-32(33)28(6-7-34(33,37)29(35)25-26)45-24-23-44-22-21-43-20-19-42-18-17-41-16-15-40-14-13-39-12-11-38-2;3-1(4)2(5)6/h3-5,28-29,32,36-37H,1,6-25H2,2H3;(H,3,4)(H,5,6)/t28-,29+,32-,33-,34+;/m0./s1

 

Smiles Code:

O[C@@]12CC[C@H](OCCOCCOCCOCCOCCOCCOCCOC)[C@@]3([H])[C@@]14CCN(CC=C)[C@]2([H])CC5=C4C(O3)=C(O)C=C5.O=C(O)C(O)=O

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO, DMF, PBS, or EtOH

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

 

References

 

  1. Al-Huniti N. Reply to: Letter to the Editor "Effect of Quinidine, a Strong P-Glycoprotein Inhibitor, on the Pharmacokinetics and Central Nervous System Distribution of Naloxegol". J Clin Pharmacol. 2016 Apr;56(4):508. doi: 10.1002/jcph.674. PubMed PMID: 26954553.

 

  1. Ruan X. The Effect of Quinidine, a Strong P-Glycoprotein Inhibitor, on the Pharmacokinetics and Central Nervous System Distribution of Naloxegol. J Clin Pharmacol. 2016 Apr;56(4):506-7. doi: 10.1002/jcph.651. PubMed PMID: 26954552.

 

  1. Naloxegol (Movantik) for Opioid-Induced Constipation. JAMA. 2016 Jan 12;315(2):194-5. doi: 10.1001/jama.2015.17459. PubMed PMID: 26757469.

 

  1. Bui K, Zhou D, Sostek M, She F, Al-Huniti N. Effects of CYP3A Modulators on the Pharmacokinetics of Naloxegol. J Clin Pharmacol. 2015 Dec 17. doi: 10.1002/jcph.693. [Epub ahead of print] PubMed PMID: 26678015.

 

  1. Naloxegol for opioid-induced constipation. Drug Ther Bull. 2015 Dec;53(12):138-40. doi: 10.1136/dtb.2015.12.0369. PubMed PMID: 26660436.

 

  1. Tack J, Lappalainen J, Diva U, Tummala R, Sostek M. Efficacy and safety of naloxegol in patients with opioid-induced constipation and laxative-inadequate response. United European Gastroenterol J. 2015 Oct;3(5):471-80. doi: 10.1177/2050640615604543. PubMed PMID: 26535126; PubMed Central PMCID: PMC4625753.

 

Products are for research use only. Not for human use.

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