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IPSU

  Cat. No.:  DC10295   Featured
Chemical Structure
1373765-19-5
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More than 5000 active chemicals with high quality for research!
Field of application
IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.
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].
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