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盐酸阿莫雷森特 /Almorexant HCl {[allProObj[0].p_purity_real_show]}

货号:A360660 同义名: ACT 078573 hydrochloride;Almorexant (hydrochloride)

Almorexant HCl is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.

Almorexant HCl 化学结构 CAS号:913358-93-7
Almorexant HCl 化学结构
CAS号:913358-93-7
Almorexant HCl 3D分子结构
CAS号:913358-93-7
Almorexant HCl 化学结构 CAS号:913358-93-7
Almorexant HCl 3D分子结构 CAS号:913358-93-7
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Almorexant HCl 纯度/质量文件 产品仅供科研

货号:A360660 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 OX1 receptor OX2 receptor 其他靶点 纯度
SB-408124 ++

OX1 (whole cell), Ki: 57 nM

OX1 (membrane), Ki: 27 nM

98%
SB-334867 free base 99%+
Almorexant HCl +++

OX1 receptor, IC50: 6.6 nM

++++

OX2 receptor, IC50: 3.4 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Almorexant HCl 生物活性

靶点
  • OX1 receptor

    OX1 receptor, IC50:6.6 nM

  • OX2 receptor

    OX2 receptor, IC50:3.4 nM

描述 Orexins are neuropeptides exclusively produced in the lateral hypothalamic areas. Orexin 1 receptor (OX1) and Orexin 2 receptor (OX2) are G-protein-coupled receptors that work together with orexins to regulate energy homeostasis, feeding and reward, and sleep-wake cycle. Almorexant is a dual OX1 and OX2 antagonist. It inhibited the binding of [125I]orexin-A to OX1 and OX2 overexpressed in CHO cells with IC50 values of 6.6 and 3.4nM, respectively. [3H]Almorexant binds to hOX1and hOX2 with Kd values of 1.3 and 0.17nM, respectively. Almorexant inhibited the binding of [3H]Almorexant to HEK293-hOX1 and -hOX2 cell membranes with Ki values of 4.7 and 0.9nM, respectively. Almorexant at 1μM antagonized orexin-A-induced increase of firing frequency of rat ventral tegmental area dopaminergic neurons[3]. The administration of Almorexant at 100mg/kg in a mouse binge-drinking model reduced ethanol intake compared to vehicle-treated controls. Almorexant at the doses of 50 and 100mg/kg also decreased the blood ethanol concentrations relative to the control mice[4].

Almorexant HCl 参考文献

[1]Sifferlen T, Boss C, et al. Novel pyrazolo-tetrahydropyridines as potent orexin receptor antagonists. Bioorg Med Chem Lett.

[2]Malherbe P, Borroni E, et al. Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor(OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists. Mol Pharmacol. 2009 Sep;76(3):618-31.

[3]Malherbe P, Borroni E, Pinard E, Wettstein JG, Knoflach F. Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists. Mol Pharmacol. 2009 Sep;76(3):618-31.

[4]Anderson RI, Becker HC, Adams BL, Jesudason CD, Rorick-Kehn LM. Orexin-1 and orexin-2 receptor antagonists reduce ethanol self-administration in high-drinking rodent models. Front Neurosci. 2014 Feb 25;8:33.

Almorexant HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.02mL

0.40mL

0.20mL

10.10mL

2.02mL

1.01mL

20.20mL

4.04mL

2.02mL

Almorexant HCl 技术信息

CAS号913358-93-7
分子式C29H35ClN2O3
分子量 495.05
别名 ACT 078573 hydrochloride;Almorexant (hydrochloride);ACT 078573;ACT-078573 HCl;Almorexant hydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

溶解度

DMSO: 45 mg/mL(90.9 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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