IPSU

Cas No.:	1373765-19-5
SMILES:	COC1=CC=NC(N(CC2)CCC2(C3=O)CCCN3CC4=CNC5=CC=CC=C54)=N1
Formula:	C23H27N5O2
M.Wt:	405.49
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.
In Vivo:	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].
In Vitro:	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].