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KP136  ≥98%

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
产品描述：基本信息 产品编号： K10175 产品名称： KP136 CAS: 76239-32-2   储存条件 粉末 -20℃ 四年 分子式： C16H18N4O3 溶于液体 -80℃ 二年 分子量： 314.34     化学名：  8-(Hexyloxy)-3-(1H-tetrazol-5-yl)-2H-1-benzopyran-2-one 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。 生物活性 产品描述 一种有效的，具有口服活性的抗过敏剂。抑制组胺释放和细胞脱粒。 靶点 Histamine release   体外研究 KP136 (0.01μg/mL) inhibits this histamine release and degranulation in a dose-dependent manner,confirming that it is an inhibitor of mast cell activation.The IC50 is 76.1μg/mL for histamine release and 63ug/mL for degranulation. 体内研究 C4C at 0.2mg/kg produces an equipotent effect to 1mg/kg KP136 (KP-136) or 5mg/kg DSCG.However,C4C is less effective by the oral route because it only produces a maximum inhibition of about 35% even at the high dose of 100mg/kg,whereas KP136 shows an overt inhibitory effect of about 66% at the oral dose of 2mg/kg.On the other hand,KP136 (1mg/kg,i.v.) also remarkably inhibits 5-h homologous PCA,having an activity similar to that of C4C. 推荐实验方法(仅供参考) 动物实验:   Pigs The trachea is taken from male guinea pigs,weighing 500-590g,that are sacrificed by bleedingand then cut into 1.5mm wide to make tracheal rings.Five specimens are tied at cartilage sites crossing each smooth muscle layer.This preparation is incubated in Tyrode's solution at 37℃,which is bubbled with 95% O2/5% CO2.The tension change of the tracheal muscle preparation is recorded through an isotonic transducer.C4C and KP136 in 0.5% KHCO3 or isoproterenol in saline is added cumulatively to the Tyrode's solution at a 1/200 volume.Relaxation percentage is calculated from the maximum relaxation value (100%) produces by re placement of the bathing medium with Tyrode's solution containing no CaCl2.
保存条件：-20℃

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