IPSU

Name	IPSU
Synonyms	IPSU 2-(1H-Indol-3-ylmethyl)-9-(4-methoxy-2-pyrimidinyl)-2,9-diazaspiro[5.5]undecan-1-one 2-((1H-indol-3-yl)methyl)-9-(4-methoxypyrimidin-2-yl)-2,9-diazaspiro[5.5]undecan-1-one 2,9-Diazaspiro[5.5]undecan-1-one, 2-(1H-indol-3-ylMethyl)-9-(4-Methoxy-2-pyriMidinyl)-
CAS	1373765-19-5
EINECS	604-604-1

Molecular Formula	C23H27N5O2
Molar Mass	405.49
Density	1.32±0.1 g/cm3(Predicted)
Boling Point	702.0±70.0 °C(Predicted)
Solubility	DMSO: ≥ 30 mg/mL
pKa	16.94±0.30(Predicted)
Storage Condition	-20℃
In vitro study	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.
In vivo study	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 .

Last Update：2024-01-02 23:10:35

biological activity	IPSU is a selective, orally active and brain-permeable OX2R antagonist with a pKi value of 7.85.
Target	pKi: 7.85 (OX2R), 6.29 (OX1R)

Last Update：2024-04-09 21:11:58

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CAS: 1373765-19-5
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Email: 3008007409@qq.com
Mobile: 18021002903
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