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CAS No.: 913358-93-7

Almorexant HCl/盐酸阿莫雷森特 Catalog No. CSN13780

Synonyms: ACT 078573 hydrochloride;ACT-078573 HCl;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.

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技术信息

生物活性

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 K_d values of 1.3 and 0.17nM, respectively. Almorexant inhibited the binding of [³H]Almorexant to HEK293-hOX1 and -hOX2 cell membranes with K_i 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].
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0200 mL
- 10.0999 mL
- 20.1999 mL
- 5 mM
- 0.4040 mL
- 2.0200 mL
- 4.0400 mL
- 10 mM
- 0.2020 mL
- 1.0100 mL
- 2.0200 mL

技术信息

CAS号

913358-93-7

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H35ClN2O3

运输

蓝冰

分子量

495.05

别名

ACT 078573 hydrochloride;ACT-078573 HCl;Almorexant (hydrochloride);ACT-078573;Almorexant;Almorexant HCl

溶解度

DMSO	72.0 mg/mL (145.4 mM)
Water	Insoluble
Ethanol	50.0 mg/mL (101.0 mM)

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Almorexant HCl/盐酸阿莫雷森特 Catalog No. CSN13780

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