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PF-06826647

CAS No. : 2127109-84-4

MCE 站：PF-06826647

产品活性：PF-06826647 是一种口服活性和选择性 TYK2 抑制剂 (IC₅₀=17 nM)，与 TYK2 催化活性 JH1 结构域结合。PF-06826647 对 JAK1 (IC₅₀=383 nM) 和 JAK2 (74 nM)具有选择性。PF-06826647 可用于银屑病、溃疡性结肠炎和化脓性汗腺炎的研究。

研究领域：Epigenetics  |  Stem Cell/Wnt  |  JAK/STAT Signaling

作用靶点：JAK

In Vitro: PF-06826647 inhibits a panel of 231 kinases at non-physiologically conditions for each kinase Km showed 21 non-JAK kinases with >50% at 1 μM dose.

In Vivo: PF-06826647 (30, 10, 3 mg/kg, p.o.; once per day) reduces clinical end points associated with the mouse imiquimod-induced skin inflammation model. The measured average unbound daily concentrations of 1, 3, 10, and 30 mg/kg are 14.5, 45.7, 225, and 668 nM, respectively, resulting in average IL-12 inhibition of 51, 77, 94, and 98%.
PF-06826647 (1 mg/kg; i.v.; sprague-Dawley rats) shows the systemic clearance is 12 (mL/min)/kg, the steady state volume of distribution (V_ss) is 1.1 L/kg, and the AUC_inf is 1380 ng?h/ mL.

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