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Almorexant HCl

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Chemical Structure| 913358-93-7 同义名 : ACT 078573 hydrochloride;Almorexant (hydrochloride);ACT 078573;ACT-078573 HCl;Almorexant hydrochloride
CAS号 : 913358-93-7
货号 : A360660
分子式 : C29H35ClN2O3
纯度 : 99%+
分子量 : 495.05
MDL号 : MFCD14636620
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
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：
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].
实验方案
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
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.