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Almorexant hydrochloride Sale

(Synonyms: 阿莫伦特盐酸盐,ACT 078573 hydrochloride) 目录号 : GC10050

An orexin 1 and orexin 2 receptor antagonist

Almorexant hydrochloride Chemical Structure

Cas No.:913358-93-7

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,576.00
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2mg
¥882.00
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5mg
¥1,305.00
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10mg
¥2,205.00
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50mg
¥7,695.00
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100mg
¥13,050.00
现货

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Sample solution is provided at 25 µL, 10mM.

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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. 913358-93-7 SDF
别名 阿莫伦特盐酸盐,ACT 078573 hydrochloride
化学名 (R,Z)-2-((R)-6,7-dimethoxy-1-(4-(trifluoromethyl)phenethyl)-3,4-dihydroisoquinolin-2(1H)-yl)-N-methyl-2-phenylacetimidic acid hydrochloride
Canonical SMILES C/N=C(O)/[C@@](N1CCC2=CC(OC)=C(OC)C=C2[C@@]1([H])CCC3=CC=C(C(F)(F)F)C=C3)([H])C4=CC=CC=C4.Cl
分子式 C29H32ClF3N2O3 分子量 549.02
溶解度 DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS(pH 7.2) (1:2): 0.25 mg/ml,Ethanol: 10 mg/ml 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mM 1.8214 mL 9.1071 mL 18.2143 mL
5 mM 0.3643 mL 1.8214 mL 3.6429 mL
10 mM 0.1821 mL 0.9107 mL 1.8214 mL
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