Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Almorexant hydrochloride (ACT-078573 hydrochloride) 是一种有效的竞争性食欲素 1 受体(OX1)/食欲素 2 受体 (OX2) 双重拮抗剂,OX1 和 OX2 的 Ki 值分别为 1.3 和 0.17 nM。
产品描述 | Almorexant hydrochloride (ACT-078573 hydrochloride) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively. |
靶点活性 | OX2:0.17 nM(ki), OX1:1.3 nM(ki) |
体外活性 | 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] |
体内活性 | 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] |
别名 | ACT-078573 hydrochloride, Almorexant HCl |
分子量 | 549.02 |
分子式 | C29H32ClF3N2O3 |
CAS No. | 913358-93-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 48 mg/mL (87.4 mM)
DMSO: 67 mg/mL (122 mM)
H2O: <1 mg/mL
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.8214 mL | 9.1071 mL | 18.2143 mL | 45.5357 mL |
5 mM | 0.3643 mL | 1.8214 mL | 3.6429 mL | 9.1071 mL | |
10 mM | 0.1821 mL | 0.9107 mL | 1.8214 mL | 4.5536 mL | |
20 mM | 0.0911 mL | 0.4554 mL | 0.9107 mL | 2.2768 mL | |
50 mM | 0.0364 mL | 0.1821 mL | 0.3643 mL | 0.9107 mL | |
DMSO | 100 mM | 0.0182 mL | 0.0911 mL | 0.1821 mL | 0.4554 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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