Almorexant hydrochloride
(Synonyms: 阿莫伦特盐酸盐,ACT 078573 hydrochloride) 目录号 : GC10050
An orexin 1 and orexin 2 receptor antagonist
Cas No.:913358-93-7
Sample solution is provided at 25 µL, 10mM.
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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.
| 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 |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 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。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet