Hydroxyzine 2HCl

製品コードS4026 バッチS402601

印刷

化学情報

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

C21H27ClN2O2.2HCl
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）
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.
Clear solution
Saline

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 30.000mg/ml (66.99mM) Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results. 
* <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 HydroxyzineはヒスタミンH1受容体拮抗薬であり、[3H]ピリラミン/[3H]デスロラタジンがヒトヒスタミンH1受容体への結合をIC50 10 nM/19 nMで阻害します。
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. 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). 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.
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. 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.

プロトコル(参考用のみ)

キナーゼアッセイ Binding assay
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

参考

  • https://pubmed.ncbi.nlm.nih.gov/12167464/
  • https://pubmed.ncbi.nlm.nih.gov/9839659/
  • https://pubmed.ncbi.nlm.nih.gov/10884588/
  • https://pubmed.ncbi.nlm.nih.gov/11290874/
  • https://pubmed.ncbi.nlm.nih.gov/523173/

カスタマーフィードバック

Data from [Data independently produced by , , Nature, 2018, 560(7718):372-376]

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：

Hydroxyzine Effects on Post-Lanosterol Biosynthesis in Smith-Lemli-Opitz Syndrome (SLOS) Models [ Biomolecules, 2025, 15(4)562] PubMed: 40305315
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。

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