受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C21H27ClN2O2.2HCl |
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分子量 | 447.83 | CAS No. | 2192-20-3 | ||||
Solubility (25°C)* | 体外 | DMSO | 90 mg/mL (200.96 mM) | ||||
Water | 90 mg/mL (200.96 mM) | ||||||
Ethanol | 15 mg/mL (33.49 mM) | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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. |
製品説明 | Hydroxyzine is a histamine H1-receptor antagonist, inhibits binding of [3H]pyrilamine/[3H]desloratadine to human histamine H1 receptor with IC50 of 10 nM/19 nM. |
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in vitro | Hydroxyzine inhibits carbachol (10 μM)-induced serotonin release by 34% at 10 μM, by 25% 1 μM and by 17% 0.1 μM in pretreated bladder slices for 60 min. [2] Hydroxyzine (0.1 mM) treatment inhibits the progression and severity of EAE by 50% and the extent of mast cell degranulation by 70% in Lewis rats with allergic encephalomyelitis (EAE). [3] Hydroxyzine (500 µM) significantly increases transport of etoposide to the serosal site in the jejunal everted sacs. Hydroxyzine significantly reduces the efflux and approximately 2.4 µg/mL of etoposide in the jejunum and ileum. Hydroxyzine (0.2 μg/mL) significantly enhances the efflux of RH123 to the lumen. [4] |
in vivo | Hydroxyzine (500 μM) significantly decreases the steady-state etoposide concentration 2-fold, where the steady-state concentration reached about 0.055 μM/mL in Sprague-Dawley rats. [4] Hydroxyzine (12.5 mg/kg, 25 mg/kg and 50 mg/kg i.p.) shows little direct analgesic activity but markedly potentiates only the effect of morphine on the vocalization after-discharge which represents the affective component of pain in rats. Hydroxyzine (50 mg/kg i.p.) potentiates morphine on the tail-flick test, while Hydroxyzine (12.5 mg/kg i.p.) decreases morphine antinociception in rats. [5] |
キナーゼアッセイ | Binding assay | |
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Membrane (5 to 10 μg of protein) is incubated with various concentrations of [3H]desloratadine (saturation binding experiments) or 2 nM [3H]pyrilamine or [3H]desloratadine (competition binding) without or with Hydroxyzine in a total volume of 200 μL of binding buffer (50 mM Tris–HCl, pH 7.5). Nonspecific binding is determined in the presence of 1 μM chlorpheniramine. Assay mixtures are incubated for 60 min at room temperature in polypropylene, 96-well, deep-well plates and then filtered through 0.3% polyethylenimine-soaked GF/B filters. These are washed three times with 1.2 mL Tris buffer, dried in a microwave oven, impregnated with Meltilex wax scintillant, and counted at 40% efficiency in a Betaplate scintillation counter. | ||
動物実験 | 動物モデル | Sprague-Dawley rats |
投薬量 | 50 mg/kg | |
投与方法 | Intraperitoneal injection |
Data from [Data independently produced by , , Nature, 2018, 560(7718):372-376]
Histamine Receptor Antagonists, Loratadine and Azelastine, Sensitize P-gp-overexpressing Antimitotic Drug-resistant KBV20C Cells Through Different Molecular Mechanisms. [ Anticancer Res, 2019, 39(7):3767-3775] | PubMed: 31262903 |
Accumulation of 8,9-unsaturated sterols drives oligodendrocyte formation and remyelination [Hubler Z, et al. Nature, 2018, 560(7718):372-376] | PubMed: 30046109 |
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。