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WHI-P97  ≥98%

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包装规格：100mg in glass bottle
溶解性：溶于DMSO（5.88mg/mL 超声）
产品描述：基本信息 产品编号： W10039 产品名称： WHI-P97 CAS: 211555-05-4   储存条件 粉末 -20℃ 四年     分子式： C16H13Br2N3O3 溶于液体 -80℃ 6个月 分子量： 329.39 -20℃ 1个月 化学名：  WHI-P 974-(3',5'-Dibromo-4-hydroxyphenyl)amino-6,7-dimethoxyquinazoline Solubility (25°C)：   体外:   DMSO 8mg/mL (17.57mM) Ethanol Insoluble Water Insoluble 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 2.1973mL 10.9866mL 21.9732mL 5mM 0.4395mL 2.1973mL 4.3946mL 10mM 0.2197mL 1.0987mL 2.1973mL   生物活性 产品描述 一种有效的选择性JAK-3抑制剂。WHI-P97在动物模型中有效预防过敏性哮喘的发展。 靶点 JAK3 11μM (IC50)   体外研究 WHI-P97 inhibits the translocation of 5-lipoxygenase (5-LO) from the nucleoplasm to the nuclear membrane and consequently 5-LO-dependent leukotriene (LT) synthesis after IgE receptor/FcεRI crosslinking by >90% at low micromolar concentrations.WHI-P97 (30μM) stantially reduces the IgE/antigen-induced LTC4 release from mast cells. 体内研究 WHI-P97 is very well tolerated in mice, with no signs of toxicity at dose levels ranging from 5μg/kg to 50mg/kg,and LD10 is not reached at a 50mg/kg dose level when administered as a single i.p.or i.v.bolus dose.WHI-P97 (i.v.injection;40mg/kg;single dose) has an elimination half-life (t1/2) of 58.9 min and systemic clearance (CL) of 891ml/h/kg in CD-1 mice and a t1/2 of 84.2 min and CL of 1513ml/h/kg in BALB/c mice.The values for AUC and Cmax are 107.3μM and 296.7μM,respectively, in CD-1 mice.And the IC50 values are 58.4μM and 212.7μM,respectively, in BALB/c mice.The large volume of distribution are 322ml/kg in CD-1 mice and 415 ml/kg in BALB/c mice.WHI-P97 (intraperitoneal injection;40mg/kg;24 days) prevents ovalbumin-sensitized mice the development of airway hyper-responsiveness to methacholine in a dose-dependent fashion in mice. WHI-P97 inhibits the eosinophil recruitment to the airway lumen after the ovalbumin challenge in a dose-dependent fashion. Animal Model: BALB/c mouse model of allergic asthma Dosage: 40mg/kg Administration: intraperitoneal injection;24 days Result: Showed promising biological activity in a mouse model of allergic asthma at nontoxic dose levels.
保存条件：-20℃

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