IPSU is a selective, orally available and brain penetrantOX2Rantagonist with apK_iof 7.85.

pKi: 7.85 (OX2R), 6.29 (OX1R)^[1]

Orexin receptor antagonists represent attractive targets for the development of drugs for the treatment of insomnia. IPSU binds rapidly and reaches equilibrium very quickly in binding and/or functional assays^[2].

IPSU has low blood clearance, shows high maximal blood exposure and AUC after oral dosing. It exhibits an acceptable absolute oral bioavailability and a brain/blood concentration ratio that indicated favorable brain penetration. IPSU increases sleep when dosed during the mouse active phase (lights off); IPSU induces sleep primarily by increasing NREM sleep. IPSU shows a fast onset of action, with a clear increase in total sleep time during the first hour afterdosing. The effect lasts 4-5 h, after which time the total sleep time per hour is the same as on vehicle day^[1].

405.49

Solid

C₂₃H₂₇N₅O₂

1373765-19-5

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 30 mg/mL(73.98 mM)

*"≥" means soluble, but saturation unknown.

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