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• 产品描述： TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model

• 靶点： p38α：7.1 nM (IC50)；p38β：200 nM (IC50)；p38δ：>10 μM (IC50)；p38γ：>10 μM (IC50)；CK1δ；CK1ε ;p38MAPK;CaseinKinase;JNK

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

• 参考文献：
  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), 5966-5979. 2. Verkaar F, et al. Inhibition of Wnt/β-catenin signaling by p38 MAP kinase inhibitors is explained by cross-reactivity with casein kinase Iδ/ɛ. Chem Biol, 2011, 18(4), 485-494. 3. Huiwen Ren, et al. Inhibition of α1-adrenoceptor reduces TGF-β1-induced epithelial-to-mesenchymal transition and attenuates UUO-induced renal fibrosis in mice. FASEB J. 2020 Nov;34(11):14892-14904.

• 溶解性： DMSO  :  ≥  100  mg/mL  (250.31  mM)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.503 ml	12.515 ml	25.031 ml
  5 mM	0.501 ml	2.503 ml	5.006 ml
  10 mM	0.25 ml	1.252 ml	2.503 ml
  50 mM	0.05 ml	0.25 ml	0.501 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *