NKTR-181( NKTR 181 | NKTR181 | Loxicodegol )

Catalog No. M10788 CAS No. 1211231-76-3

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Product Name

NKTR-181
Note

Research use only, not for human use.
Brief Description

A novel, long-acting and orally active, selective mu-opioid agonist.
Description

A novel, long-acting and orally active, selective mu-opioid agonist that displays higher binding affinity (Ki=237 nM) at the MOR than kappa and delta opioid receptors (>100-fold); demonstrates maximum analgesic activity comparable to that of oxycodone in hot-plate latency and acetic-acid writhing models, reduces its rate of entry across the blood-brain barrier compared with traditional mu-opioid agonists.Pain Phase 3 Clinical.
In Vitro

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In Vivo

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Synonyms

NKTR 181 | NKTR181 | Loxicodegol
Pathway

Endocrinology/Hormones
Target

Opioid Receptor
Recptor

Opioid Receptor
Research Area

Neurological Disease
Indication

Pain

CAS Number

1211231-76-3
Formula Weight

595.73
Molecular Formula

C31H49NO10
Purity

>98% (HPLC)
Solubility

——
SMILES

O[C@]1([C@H](N(C)CC2)C3)[C@@]42C5=C3C=CC(OC)=C5O[C@H]4[C@@H](OCCOCCOCCOCCOCCOCCOC)CC1
Chemical Name

(4R,4aS,7S,7aR,12bS)-7-((2,5,8,11,14,17-hexaoxanonadecan-19-yl)oxy)-9-methoxy-3-methyl-1,2,3,4,5,6,7,7a-octahydro-4aH-4,12-methanobenzofuro[3,2-e]isoquinolin-4a-ol

1. Miyazaki T, et al. J Pharmacol Exp Ther. 2017 Oct;363(1):104-113. 2. Webster L, et al. Pain Med. 2017 Mar 10. doi: 10.1093/pm/pnw344.

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