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Almorexant Sale

(Synonyms: 阿莫伦特; ACT 078573) 目录号 : GC10717

Almorexant (ACT 078573) 是一种具有口服活性、强效和竞争性的双重食欲素受体拮抗剂,Kd 值分别为 1.3 nM (OX1) 和 0.17 nM (OX2)。

Almorexant Chemical Structure

Cas No.:871224-64-5

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5mg
¥861.00
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10mg
¥1,586.00
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50mg
¥5,240.00
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产品描述

Almorexant is an antagonist of Orexin 1 receptor (OX1R) and Orexin 2 receptor (OX2R) with Kd values of 1.3nM and 0.17nM, respectively [1].

Almorexant is a dual OX antagonist. It inhibits the binding of orexin-A to both OX1R and OX2R with IC50 values of 6.6nM and 3.4nM, respectively. In the inositol phosphates assay, almorexant acts as a competitive antagonist of hOX1R but a noncompetitive-like antagonist of hOX2R. Besides that, almorexant is found to block the increase in locomotor activity induced by ICV orexin in C57BL/6 mice. Furthermore, almorexant shows effects on sleep in multiple species, including man. It reduces the time spent awake and increased the time spent in NREM and REM sleep dose-dependently in normal C57BL/6 mice. These effects on sleep caused by almorexant are mediated by OX2Rs as almorexant has no effect in mice lacking both OX1R and OX2R but has effects in mice lacking only OX1R [1, 2].

References:
[1] 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.
[2] Mang GM1, Dürst T, Bürki H, Imobersteg S, Abramowski D, Schuepbach E, Hoyer D, Fendt M, Gee CE. The dual orexin receptor antagonist almorexant induces sleep and decreases orexin-induced locomotion by blocking orexin 2 receptors. Sleep. 2012 Dec 1;35(12):1625-35.

Chemical Properties

Cas No. 871224-64-5 SDF
别名 阿莫伦特; ACT 078573
化学名 (2R)-2-[(1S)-6,7-dimethoxy-1-[2-[4-(trifluoromethyl)phenyl]ethyl]-3,4-dihydro-1H-isoquinolin-2-yl]-N-methyl-2-phenylacetamide
Canonical SMILES CNC(=O)C(C1=CC=CC=C1)N2CCC3=CC(=C(C=C3C2CCC4=CC=C(C=C4)C(F)(F)F)OC)OC
分子式 C29H31F3N2O3 分子量 512.56
溶解度 Soluble in DMSO 储存条件 Desiccate at -20°C
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1 mM 1.951 mL 9.755 mL 19.5099 mL
5 mM 0.3902 mL 1.951 mL 3.902 mL
10 mM 0.1951 mL 0.9755 mL 1.951 mL
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