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TAK-715
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
TAK-715图片
CAS NO:303162-79-0
包装与价格：
包装价格(元)
5mg电议
10mg电议
50mg电议
500mg电议
1g电议

产品介绍
TAK-715 是一种口服有效的 p38 MAPK 抑制剂，对 p38α 和 p38β 的 IC50 分别为 7.1 nM 和 200 nM。
Cas No.303162-79-0
别名N-(4-(2-乙基-4-(3-甲基苯基)噻唑-5-基)吡啶-2-基)苯甲酰胺
化学名N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]pyridin-2-yl]benzamide
Canonical SMILESCCC1=NC(=C(S1)C2=CC(=NC=C2)NC(=O)C3=CC=CC=C3)C4=CC(=CC=C4)C
分子式C24H21N3OS
分子量399.52
溶解度≥ 40mg/mL in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

TAK-715 is a selective inhibitor of p38 MAPK with IC50 value of 7.1 nM [1].

p38 mitogen-activated protein (MAP) kinases (p38 MAPKs) are a class of mitogen-activated protein kinases and play an important role in controlling cellular responses to cytokines and stress. Four p38 MAPKs contain members, p38-α (MAPK14), p38-β (MAPK11), p38-γ (MAPK12/ERK6), and p38-δ (MAPK13/SAPK4), have been identified. Abnormal expression of p38 MAPKs are correlated with a variety of chronic inflammatory diseases and their inhibitors are regarded as promising targets in clinical [1] [2].

TAK-715 is a potent p38 MAPK inhibitor and has a different selectivity with the reported p38 MAPK inhibitor VX-745. When tested with human monocytic THP-1 cells, administration of TAK-715 exhibited inhibition on p38MAPKα with IC50 value of 7.1 nM [1]. In HEK293T, U2OS, and F9 cells, TAK-715 was used to inhibit p38 MAPK activity and concluded that p38 MAPK had no function in Wnt/β-catenin signaling pathway [2].

In adjuvant-induced rheumatoid arthritis rat model, administration of TAK-715 at dose of 10 mg/kg significantly decreased LPS-induced stimulated release of TNF-α (87.6%) by inhibiting p38 MAPK activity [1].

References:
[1].  Miwatashi, S., et al., Novel inhibitor of p38 MAP kinase as an anti-TNF-alpha drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent. J Med Chem, 2005. 48(19): p. 5966-79.
[2].   Verkaar, F., et al., Inhibition of Wnt/beta-catenin signaling by p38 MAP kinase inhibitors is explained by cross-reactivity with casein kinase Idelta/varepsilon. Chem Biol, 2011. 18(4): p. 485-94.