Nemorexant (ACT-541468)是一种苯并咪唑衍生物，是一种口服选择性双重orexin受体拮抗剂（DORA）。
Cas No.:1505484-82-1
Sample solution is provided at 25 µL, 10mM.
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Nemorexant (ACT-541468), a benzimidazole derivative, is an orally selective dual-orexin antagonist (DORA) [1]. Nemorexant can cross the blood-brain-barrier (BBB) and work by competitively binding to the active site of orexin 1 and orexin 2 receptors[2]. Nemorexant has been widely used to reduce the arousal state and promote sleep in animals, and to maintain overall sleep architecture[3].
In vivo, Nemorexant treatment via oral administration at a dose of 200mg/kg/day for 14 days reduced the body temperature of the rats, resulting in decreased locomotor activity and a lower level of vertical activity[4]. Oral administration of Nemorexant (100mg/kg/day) for three consecutive days prior to lipopolysaccharide (LPS) injection enhanced rapid eye‐movement (REM) sleep recovery, and decreased the expression of proinflammatory cytokines (Cxcl1, Ccl2, Ccl7, and Tnf) in the hypothalamus in the LPS-induced systemic inflammation model[5].
References:
[1] Ziemichód W, Grabowska K, Kurowska A, et al. A comprehensive review of daridorexant, a dual-orexin receptor antagonist as new approach for the treatment of insomnia[J]. Molecules, 2022, 27(18): 6041.
[2] Robinson C L, Supra R, Downs E, et al. Daridorexant for the Treatment of Insomnia[J]. Health psychology research, 2022, 10(3): 37400.
[3] Roch C, Bergamini G, Steiner M A, et al. Nonclinical pharmacology of daridorexant: a new dual orexin receptor antagonist for the treatment of insomnia[J]. Psychopharmacology, 2021, 238(10): 2693-2708.
[4] Steiner M A, Toeroek-Schafroth M, Giusepponi M E, et al. Abuse potential assessment of the dual orexin receptor antagonist daridorexant in rats[J]. Journal of Psychopharmacology, 2023, 37(12): 1249-1260.
[5] Horiuchi D, Irukayama‐Tomobe Y, Kim J D, et al. Orexin Receptor Antagonism Improves Sleep Quality and Mitigates Lipopolysaccharide‐Induced Inflammatory Responses in a Mouse Model[J]. The FASEB Journal, 2026, 40(1): e71408.
Nemorexant (ACT-541468)是一种苯并咪唑衍生物，是一种口服选择性双重orexin受体拮抗剂（DORA）[1]。Nemorexant可穿过血脑屏障（BBB），通过竞争性结合orexin 1和orexin 2受体的活性位点发挥作用[2]。Nemorexant已被广泛用于降低动物的觉醒状态、促进睡眠，并维持整体的睡眠结构[3]。
在体内，每日口服给予200mg/kg剂量的Nemorexant，持续14天，降低了大鼠的体温，导致自主活动减少和垂直活动水平降低[4]。在脂多糖（LPS）注射前连续三天口服给予Nemorexant（100mg/kg/day），在LPS诱导的全身炎症模型中，增强了快速眼动（REM）睡眠的恢复，并降低了下丘脑中促炎细胞因子（Cxcl1、Ccl2、Ccl7和Tnf）的表达[5]。
| Animal experiment [1]: | |
Animal models | Male C57BL/6J mice |
Preparation Method | Male C57BL/6J mice, aged 8-15 weeks, were housed in an animal experimental facility under specific pathogen‐free conditions in plastic cages at 23°C±1°C with a 12h light/dark cycle. Mice had unrestricted access to food and drinking water. Systemic inflammation was induced in mice through the peritoneal injection of LPS at a dose of 2.5mg/kg. The mice received oral administration of Nemorexant (100mg/kg) or vehicle for three consecutive days before LPS injection. The mice were randomly assigned to four groups: LPS+vehicle (LPS group), LPS+ Nemorexant group, saline+vehicle (Vehicle group), and saline+Nemorexant (Nemorexant group). Mice hypothalamic tissues were collected for analysis. |
Dosage form | 100mg/kg/day for 3 days; p.o. |
Applications | Nemorexant treatment mitigated LPS‐induced inflammatory responses by suppressing the expression of pro‐inflammatory genes in the hypothalamus of mice. |
References: | |
| Cas No. | 1505484-82-1 | SDF | |
| 别名 | 奈莫雷生 | ||
| Canonical SMILES | C[C@](CCC1)(C2=NC3=CC=C(Cl)C(C)=C3N2)N1C(C4=C(N5N=CC=N5)C=CC(OC)=C4)=O | ||
| 分子式 | C23H23ClN6O2 | 分子量 | 450.92 |
| 溶解度 | DMSO : ≥ 250 mg/mL (554.42 mM) | 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 | 2.2177 mL | 11.0884 mL | 22.1769 mL |
| 5 mM | 443.5 μL | 2.2177 mL | 4.4354 mL |
| 10 mM | 221.8 μL | 1.1088 mL | 2.2177 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。
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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