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Orexin 2 Receptor Agonist

Names

[ CAS No. ]:
1796565-52-0

[ Name ]:
Orexin 2 Receptor Agonist

[Synonym ]:
Benzamide, N-[2-[[3-[[[3'-[(dimethylamino)carbonyl]-4-methoxy[1,1'-biphenyl]-3-yl]sulfonyl]amino]phenyl]amino]ethyl]-3-methyl-
4'-Methoxy-N,N-dimethyl-3'-{[3-({2-[(3-methylbenzoyl)amino]ethyl}amino)phenyl]sulfamoyl}-3-biphenylcarboxamide
Orexin 2 Receptor Agonist
MDK-5220

Biological Activity

[Description]:

Orexin 2 Receptor Agonist is a potent (EC50 on OX2R is 23 nM) and OX2R-selective (OX1R/OX2R EC50 ratio is 70) agonist.IC50 value: 23 nM (EC50)Target: Orexin 2 ReceptorOrexin 2 Receptor Agonist shows not only potentactivity but also high selectivity for OX2R over OX1R. In CHO cells overexpressing hOX1R and HEK-293 cells overexpressing hOX2R, compound 26 displaced [125I]orexin-A in a concentration dependent manner: 26 bound to hOX2R and hOX1R with Ki of 0.14 and 0.77 μM, respectively.[1]

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Orexin Receptor (OX Receptor)
Research Areas >> Neurological Disease

[References]

[1]. Nagahara T, et al. Design and Synthesis of Non-Peptide, Selective Orexin Receptor 2 Agonists. J Med Chem. 2015 Oct 22;58(20):7931-7.


[Related Small Molecules]

SB 334867 | lemborexant | Almorexant HCI | Filorexant | TCS-OX2-29 | MK-1064 | SB-674042 | GSK1059865 | IPSU | SB408124 | MK-3697 | Nemorexant | Orexin B (mouse, rat) | SB-649868 | TCS 1102

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Molecular Formula ]:
C32H34N4O5S

[ Molecular Weight ]:
586.701

[ Exact Mass ]:
586.224976

[ LogP ]:
3.40

[ Index of Refraction ]:
1.629

[ Storage condition ]:
2-8℃

Related Compounds