CAS NO: | 211555-05-4 |
生物活性 | WHI-P97 is a potent and selectiveJAK-3inhibitor. WHI-P97 is effective in preventing the development allergic asthma in vivo[1]. | ||||||||||||||||
IC50& Target |
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体外研究 (In Vitro) | 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[1].WHI-P97 (30 μM) stantially reduces the IgE/antigen-induced LTC4 release from mast cells[1]. | ||||||||||||||||
体内研究 (In Vivo) | WHI-P97 is very well tolerated in mice, with no signs of toxicity at dose levels ranging from 5 μg/kg to 50 mg/kg, and LD10is not reached at a 50 mg/kg dose level when administered as a single i.p. or i.v. bolus dose[1].WHI-P97 (i.v. injection; 40 mg/kg; single dose) has an elimination half-life (t1/2) of 58.9 min and systemic clearance (CL) of 891 ml/h/kg in CD-1 mice and a t1/2of 84.2 min and CL of 1513 ml/h/kg in BALB/c mice. The values for AUC and Cmaxare 107.3 μM and 296.7 μM, respectively, in CD-1 mice. And the IC50values are 58.4 μM and 212.7 μM, respectively, in BALB/c mice. The large volume of distribution are 322 ml/kg in CD-1 mice and 415 ml/kg in BALB/c mice[1].WHI-P97 (intraperitoneal injection; 40 mg/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[1].
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分子量 | 455.10 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C16H13Br2N3O3 | ||||||||||||||||
CAS 号 | 211555-05-4 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 3.33 mg/mL(7.32 mM;ultrasonic and warming and heat to 80℃) 配制储备液
* 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。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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