WHI-P97,211555-05-4

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WHI-P97

CAS No. : 211555-05-4

MCE 国际站：WHI-P97

产品活性：WHI-P97 是一种有效的选择性 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。

研究领域：Epigenetics  |  Protein Tyrosine Kinase/RTK  |  JAK/STAT Signaling  |  Stem Cell/Wnt

作用靶点：JAK

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.
WHI-P97 (30 μM) stantially reduces the IgE/antigen-induced LTC4 release from mast cells.

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 LD₁₀ is not reached at a 50 mg/kg dose level when administered as a single i.p. or i.v. bolus dose.
WHI-P97 (i.v. injection; 40 mg/kg; single dose) has an elimination half-life (t_1/2) of 58.9 min and systemic clearance (CL) of 891 ml/h/kg in CD-1 mice and a t_1/2 of 84.2 min and CL of 1513 ml/h/kg in BALB/c mice. The values for AUC and C_max are 107.3 μM and 296.7 μM, respectively, in CD-1 mice. And the IC₅₀ values 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.
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.

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