貨號	規格	價格	上海	北京	武漢	南京
S83032-5mg	≥98%	￥1400.00 S83032-5mg ￥1400.00 2-3天	0 貨期：2-3天	-	-	-
S83032-10mg	≥98%	￥1800.00 S83032-10mg ￥1800.00 2-3天	0 貨期：2-3天	-	-	-
S83032-25mg	≥98%	￥3800.00 S83032-25mg ￥3800.00 2-3天	0 貨期：2-3天	-	-	-
S83032-50mg	≥98%	￥6800.00 S83032-50mg ￥6800.00 2-3天	0 貨期：2-3天	-	-	-

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產品介紹

IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.

產品描述：

IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.

靶點：

pKi: 7.85 (OX2R), 6.29 (OX1R);OXReceptor

體外研究：

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

體內研究：

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

參考文獻：

1. Betschart C, et al. Identification of a novel series of orexin receptor antagonists with a distinct effect on sleeparchitecture for the treatment of insomnia. J Med Chem. 2013 Oct 10;56(19):7590-607. 2. Callander GE, et al. Kinetic properties of 'dual' orexin receptor antagonists at OX1R and OX2R orexin receptors. Front Neurosci. 2013 Dec 3;7:230. 3. Hoyer D, et al. Distinct effects of IPSU and suvorexant on mouse sleep architecture. Front Neurosci. 2013 Dec 10;7:235.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.466 ml	12.331 ml	24.661 ml
5 mM	0.493 ml	2.466 ml	4.932 ml
10 mM	0.247 ml	1.233 ml	2.466 ml
50 mM	0.049 ml	0.247 ml	0.493 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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