IPSU

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

IPSU 是 OX2 受体拮抗剂。 IPSU 对 OX2 受体的选择性约为 OX1 受体的六倍。

IPSU is an antagonist of OX2 receptor. IPSU Exhibits approximately six-fold selectivity for OX2 versus OX1 receptors.

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.

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 .

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Others

Other Targets

OX1|OX2

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1373765-19-5

405.49

C23H27N5O2

>98% (HPLC)

DMSO : 30 mg/mL (73.98 mM)

COC1=CC=NC(N(CC2)CCC2(C3=O)CCCN3CC4=CNC5=CC=CC=C54)=N1

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(-20℃)

With Ice Pack

≥ 2 years