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TAK-715

CAS No. : 303162-79-0

MCE 国际站：TAK-715

产品活性：TAK-715 是一种具有口服活性，有效的 p38 MAPK 抑制剂，对 p38α 和 p38β 的 IC₅₀ 分别为 7.1 nM，200 nM。TAK-715 抑制酪蛋白激酶 I (CK1δ/ε)，从而调节 Wnt/β-catenin 信号传导的激活。TAK-715 在大鼠关节炎模型中显示出良好的作用。

研究领域：MAPK/ERK Pathway  |  Stem Cell/Wnt  |  Cell Cycle/DNA Damage

作用靶点：p38 MAPK  |  Casein Kinase

In Vitro: TAK-715 (compound 8h) inhibits LPS-stimulated release of TNF-α from THP-1 (IC₅₀=48 nM) and has no inhibitory activity for major CYPs, including CYP3A4. TAK-715 has no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1 (IC₅₀>10 μM of all).
TAK 715 (10 μM; 1 hour) inhibits Wnt-3a-induced hDvl2 phosphorylation and the hDvl2 shift in U2OS-EFC cells.
TAK-715 (1 μM; pretreatment for 16 hours) dramatically suppresses Norepinephrine (NE)-stimulated induction of fibronectin, CTGF, and Snai1 expression in TGF-β1-treated HK-2 cells at both the mRNA and protein levels.

In Vivo: TAK-715 (compound 8h; 3-30 mg/kg; PO) significantly reduces the secondary paw volume.
TAK-715 (10 mg/kg; PO) has a C_max of 0.19 μg/mL and an AUC of 1.16 μg h/mL.

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