货号	规格	价格	上海	北京	珠海	重庆	武汉
S85196-1mg买3赠1	99.10%	￥470.00 S85196-1mg ￥470.00 现货（买3赠1）	9 9	-	-	-	-
S85196-5mg促销	99.10%	￥1050.00 ￥840.00 S85196-5mg ￥840.00 现货	5 5	-	-	-	-
S85196-10mg促销	99.10%	￥1800.00 ￥1440.00 S85196-10mg ￥1440.00 现货	6 6	-	-	-	-
S85196-25mg促销	99.10%	￥3820.00 ￥3050.00 S85196-25mg ￥3050.00 现货	5 5	-	-	-	-

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产品描述：

SB-649868 is a potent and selective orally active orexin (OX) 1 and OX2 receptor antagonist (pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively).

靶点：

pKi: 9.4 (OX1), 9.5 (OX2);OXReceptor

体外研究：

SB-649868 is identified as one the most in vitro potent dual OX1 and OX2 receptor antagonist known at that time (pKi=9.4 and 9.5 at the OX1 and OX2 receptor, respectively) . SB-649868 antagonizes orexin-A-induced inositol 1 phosphate (IP1) accumulation with the following pKB value (OX1=9.67; OX2=9.64). SB-649868 displaces the [3H]ACT-078573 receptor binding with the following pKi values: OX1=9.27; OX2=8.91. Increasing concentrations of SB-649868 (0.3 nM-30 nM) induces a rightward shift of the orexin-A CRCs with a depression of the agonist efficacy suggesting a clear non-surmountable behavior. The calculated apparent pKb values are 9.67±0.03 and 9.64±0.07 for OX1 and OX2.

参考文献：

1. Di Fabio R, et al. Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2receptor antagonist useful for treatment of sleep disorders. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5562-7. 2. Faedo S, et al. Functional and binding kinetic studies make a distinction between OX1 and OX2 orexin receptorantagonists. Eur J Pharmacol. 2012 Oct 5;692(1-3):1-9.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.094 ml	10.47 ml	20.94 ml
5 mM	0.419 ml	2.094 ml	4.188 ml
10 mM	0.209 ml	1.047 ml	2.094 ml
50 mM	0.042 ml	0.209 ml	0.419 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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