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喹托司特钠  ≥98%

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包装规格：1mg 5mg in glass bottle
产品描述：基本信息 产品编号： Q10065 产品名称： Quinotolast sodium CAS: 101193-62-8   储存条件 粉末 -20℃ 四年 分子式： C17H12N6NaO3 溶于液体 -80℃ 二年 分子量： 371.31     化学名：  sodium;4-oxo-1-phenoxy-N-(1,2,3-triaza-4-azanidacyclopenta-2,5-dien-5-yl)quinolizine-3-carboxamide Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.6932mL 13.4658mL 26.9317mL 5mM 0.5386mL 2.6932mL 5.3863mL 10mM 0.2693mL 1.3466mL 2.6932mL   生物活性 产品描述 一种组胺抑制剂，LTC4 和 PGD2 释放，这种作用具有浓度依赖性。 靶点 Histamine LTC4 PGD2   体外研究 Quinotolast inhibits the release of histamine and the generation of leukotriene (LT) C4 and prostaglandin (PG) D2 from dispersed human lung cells.Quinotolast (100μg/mL) significantly inhibits PGD2 and LTC4 release.Quinotolast inhibits PGD2 release by 100% and LTC4 release by 54%.The inhibitory effect of Quinotolast on histamine release from dispersed lung cells is largely independent of the preincubation period,no tachyphylaxis being observed.Quinotolast shows a significant inhibition of inflammatory mediators from human dispersed lung cells.Quinotolast also shows strong inhibitory effects on histamine and peptide leukotrienes release from guinea pig lung fragments or mouse cultured mast cells.Quinotolast concentration-dependently inhibits pLTs release from cultured mast cells.The IC50 value for Quinotolast is 0.72μg/mL. 体内研究 Quinotolast potently inhibits such type I allergic reactions as passive cutaneous anaphylaxis (PCA) and anaphylactic bronchoconstriction in rats by both intravenous and oral dosing.When Quinotolast is given i.v.to rats,Quinotolast,dosedependently inhibits PCA.The doses of Quinotolast required to inhibit the reaction by 50% (ED50) is 0.0063mg/kg.Given p.o.,Quinotolast inhibits the reaction.ED50 value for Quinotolast is 0.0081mg/kg.Although almost complete inhibition is observed with Quinotolast at a dose of 0.32mg/kg,its effect is slightly attenuated at a dose of 1mg/kg.   推荐实验方法(仅供参考) 细胞实验:   Mast cells are obtained after the culture of bone marrow cells from the femurs of female BDF1 mice in the presence of conditioned medium from WEHI-3 cells containing interleukin 3.The cells are suspended with Tyrode's buffer (137mM NaCI,2.7mM KC1,1.8mM CaCl2,1mM MgCl2,0.4mM NaH2PO4,11.9mM NaHCO3,5.6mM glucose) containing 0.1% gelatin and are sensitized with mouse monoclonal anti-DNP IgE (50μg/106 cells). Then the cells are washed and resuspended with Tyrode's buffer containing 0.25% BSA.The cells (2×106 cells) are incubated for 5 min at37℃ and challenged with TNP-BSA (2ng BSA/mL).Quinotolast (0.1,1,10,100ug/mL) is added to the reaction tube simultaneously with the antigen.Ten minutes later, the reaction is stopped by the addition of EDTA (2.7mM).pLTs in the cell supernatant sre quantified as immunoreactive leukotriene C4 (iLTC4) with a leukotriene C4/D4/E4[3H] assay system.% Inhibition is calculated in each experiment from the amount of immunoreactive leukotriene C4 (iLTC4).   动物实验:   Rats Rats (8 week-old) are used.To study the presence of tachyphylaxis by Quinotolast,Quinotolast (0.001,0.01,0.1,1,10 and 100mg/kg) is given i.v.in a large dose 30 min before challenge,and again at a smaller dose simultaneously with the antigen challenge.
保存条件：-20℃

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