Desloratadine

製品コードS4012 バッチS401201

印刷

化学情報

Chemical Structure Synonyms SCH-34117, NSC 675447 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C19H19ClN2
分子量 310.82 CAS No. 100643-71-8
Solubility (25°C)* 体外 Ethanol 62 mg/mL (199.47 mM)
DMSO 26 mg/mL (83.64 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
4%DMSO 40%PEG300 4%Tween80 52%ddH2O
4.0mg/ml Taking the 1 mL working solution as an example, add 40 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 40 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 520 μL of ddH2O to adjust the volume to 1 mL. 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 Desloratadine (SCH-34117, NSC 675447) is a potent antagonist for human histamine H1 receptor with IC50 of 51 nM.
in vitro Desloratadine is a competitive antagonist of carbachol-induced contractions in isolated rabbit iris smooth muscle with pA2 of 6.67. [1] Desloratadine binds to the human H1 receptor with Ki value of 0.87 nM in displacing tritiated mepyramine. Desloratadine (100 nM to 10 μM) inhibits both IgE-mediated and non–IgE-mediated generation of the cytokines IL-4 and IL-13 by human basophils. Desloratadine (300 nM to 100 μM) inhibits both IgE and non–IgE-mediated histamine release from human peripheral blood basophils. Desloratadine (0.1 μM to 10 μM) is also shown to inhibit platelet-activating factor-induced eosinophil chemotaxis and TNF-α-induced eosinophil adhesion in eosinophils obtained from patients with allergic rhinitis or allergic asthma. [2] Desloratadine (1 μM-10 μM) dose-dependently inhibits the release of histamine and LTC4 from human basophils. Desloratadine (0.1 μM-10 μM) dose-dependently inhibits IL-13 secretion from basophils activated with IL-3 and PMA from human basophils. Desloratadine (10 μM) pretreatment results in a substantial decrease of the induced cytokine message in cultured basophils. Desloratadine (10 μM) pretreatment causes approximately an 80% reduction in the IL-4 message accumulated with anti-IgE activation in cultured basophils. Desloratadine (10 μM) also inhibits the histamine and IL-4 protein secreted into the supernatants of cultured basophils. [3] [3H]Desloratadine binds to the human histamine H1 receptor expressed in CHO cells with Kd of 1.1 nM. Desloratadine is 52, 57, 194, and 153 times more potent than cetirizine, ebastine, fexofenadine, and loratadine, respectively, in competition-binding studies. [4]
in vivo Desloratadine (1 mg/mL, 3 mg/mL and 10 mg/mL) induces a dose-dependent and long lasting mydriasis in the guinea-pig in vivo. [1] Desloratadine inhibits histamine-induced paw edema with ED50 of 0.15 mg/kg in mice. Desloratadine inhibits an increase in microvascular permeability in response to a histamine challenge to the upper airway of guinea pigs with ED50 of 0.9 μg. [2] Desloratadine (5 mg/kg) causes inhibition of oxotremorine-induced tremor by disrupting blood-brain barrier in conscious mice. Desloratadine (1.0 mg/kg) significantly inhibits oxotremorine-induced (0.00125 mg/kg, 0.0025 mg/kg, and 0.02 mg/kg) decreases in dP/dt indicated by a shift in the dose-response curve to the right in the pithed rat. Desloratadine (1.0 mg/kg) significantly inhibits oxotremorine-induced (0.00125 mg/kg, 0.0025 mg/kg, and 0.02 mg/kg) decreases in dP/dt indicated by a shift in the dose-response curve to the right in the pithed rat. [5]
特徴 Desloratadine is the active metabolite of loratadine.

プロトコル(参考用のみ)

キナーゼアッセイ Binding assays
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 desloratadine 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 10 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 Male guinea-pigs
投薬量 10 mg/kg
投与方法 Subcutaneous

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：

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

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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