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NKTR-181

Names

[ CAS No. ]:
1211231-76-3

[ Name ]:
NKTR-181

[Synonym ]:
(5α,6α)-6-(2,5,8,11,14,17-Hexaoxanonadecan-19-yloxy)-3-methoxy-17-methyl-4,5-epoxymorphinan-14-ol
Morphinan-14-ol, 4,5-epoxy-6-(3,6,9,12,15,18-hexaoxanonadec-1-yloxy)-3-methoxy-17-methyl-, (5α,6α)-
oxycodegol

Biological Activity

[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

[References]

References 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. View Related Products by Target Opioid Receptor Pain

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
679.2±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C31H49NO10

[ Molecular Weight ]:
595.721

[ Flash Point ]:
364.6±31.5 °C

[ Exact Mass ]:
595.335632

[ LogP ]:
-0.49

[ Vapour Pressure ]:
0.0±2.2 mmHg at 25°C

[ Index of Refraction ]:
1.560

Related Compounds