SB-649868 (Synonyms: GSK649868)
目录号: PL08094 纯度: ≥99%
CAS No. :380899-24-1
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中文名称
SB-649868
中文别名
(S)-N-((1-(5-(4-氟苯基)-2-甲基噻唑-4-羰基)哌啶-2-基)甲基)苯并呋喃-4-甲酰胺
英文名称
SB-649868
英文别名
SB-649868;N-[[(2S)-1-[5-(4-fluorophenyl)-2-methyl-1,3-thiazole-4-carbonyl]piperidin-2-yl]methyl]-1-benzofuran-4-carboxamide
Cas No.
380899-24-1
分子式
C26H24N3O3FS
分子量
477.55
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
SB-649868 是一种口服有效的选择性食欲素 OX1 和 OX 2 受体拮抗剂 (作用于 OX1 和 OX2 受体,pKi 分别为 9.4 和 9.5)。
生物活性
SB-649868 is a potent and selective orally active orexin (OX) 1 and OX 2 receptor antagonist (pK i =9.4 and 9.5 at the OX 1 and OX 2 receptor, respectively).
性状
Solid
IC50 & Target[1][2]
pKi: 9.4 (OX1), 9.5 (OX2)
体外研究(In Vitro)
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 [H]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. has not i
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (209.40 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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