Almorexant HCl

製品コードS2160 バッチS216001

印刷

化学情報

Chemical Structure Synonyms ACT-078573 HCl Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C29H32ClF3N2O3
分子量 549.02 CAS No. 913358-93-7
Solubility (25°C)* 体外 DMSO 72 mg/mL (131.14 mM)
Ethanol 51 mg/mL (92.89 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Almorexant HCl (ACT-078573) is an orally active, dual orexin receptor antagonist with IC50 of 6.6 nM and 3.4 nM for OX1 and OX2 receptor, respectively. Phase 3.
in vitro Almorexant inhibits the increase in intracellular Ca2+ induced by 10 nM human orexin-A in Chinese hamster ovary cells with IC50 of 16 nM (rat) and 13 nM (human) for the OX1 receptor and 15 nM (rat) and 8 nM (human) for the OX2 receptor. [1]
in vivo Almorexant (300 mg/kg p.o.) decreases alertness, and increases electrophysiological indices of both non-REM and REM sleep in male Wistar rats. In dogs, Almorexant (100 mg/kg p.o.) causes somnolence and increases surrogate markers of REM sleep. [1] Almorexant induces a robust antidepressant-like effect and the restoration of stress-related HPA axis defect independently from a neurogenic action. [2] In addition, Almorexant also reduces ethanol self-administration in high-drinking rodent models. [3]
特徴 Orally bioavailable orexin receptor antagonist that has been tested in Phase III clinical trials for treatment of Insomnia.

プロトコル(参考用のみ)

キナーゼアッセイ Selectivity screen
Almorexant is tested at a concentration of 10 μM in 89 radioligand binding or enzymatic reaction assays. For those assays in which more than 50% inhibition or stimulation is observed, the IC50 is determined.
動物実験 動物モデル Wistar rats.
投薬量 ~300 mg/kg
投与方法 p.o.

参考

  • https://pubmed.ncbi.nlm.nih.gov/17259994/
  • https://pubmed.ncbi.nlm.nih.gov/22713907/
  • https://pubmed.ncbi.nlm.nih.gov/24616657/

カスタマーフィードバック

Data from [Data independently produced by , , J Pharmacol Exp Ther, 2016, 358(3):492-501. ]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Impaired microglial glycolysis promotes inflammatory responses after intracerebral haemorrhage via HK2-dependent mitochondrial dysfunction [ J Adv Res, 2024, S2090-1232(24)00359-X] PubMed: 39142439
Mouse parasubthalamic Crh neurons drive alcohol drinking escalation and behavioral disinhibition [ bioRxiv, 2024, 2024.07.06.602357] PubMed: 39026704
Cancer genes disfavoring T cell immunity identified via integrated systems approach [ Cell Rep, 2022, 40(5):111153] PubMed: 35926468
Brain Circuit of Claustrophobia-like Behavior in Mice Identified by Upstream Tracing of Sighing [ Cell Rep, 2020, 31(11):107779] PubMed: 32553161
Optogenetic identification of hypothalamic orexin neuron projections to paraventricular spinally projecting neurons. [ Am J Physiol Heart Circ Physiol, 2017, 312(4):H808-H817] PubMed: 28159808
Intrathecal Intermittent Orexin-A Causes Sympathetic Long-Term Facilitation and Sensitizes the Peripheral Chemoreceptor Response to Hypoxia in Rats. [Kim SJ, et al. J Pharmacol Exp Ther, 2016, 358(3):492-501] PubMed: 27384072

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。