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- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
303162-79-0
- 规格：
10 mM * 1 mL/5 mg/10 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1023.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥930.0 |
| 规格： | 10 mg | 产品价格： | ￥1200.0 |
| 规格： | 50 mg | 产品价格： | ￥3700.0 |
| 规格： | 100 mg | 产品价格： | ￥5920.0 |
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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 Cmax of 0.19 μg/mL and an AUC of 1.16 μg h/mL.
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Metabolism 上在线发表了题为 Tripartite motif 16 ameliorates nonalcoholic steatohepatitis by promoting the degradation of phospho-TAK1 的研究成果 (4)。该研究发现 E3 泛素连接酶 TRIM16 通过促进 p-TAK1 的泛素化依赖性降解，改善 NASH 进展过程中的脂质积累和炎症。 图片来源：Cell Metabolism研究内容肝细胞的脂肪毒性诱导 TRIM16 的表达脂肪毒性是脂质过度积累
Smads, TAK1, and Their Common Target ATF-2 Play a Critical Role in Cardiomyocyte Differentiation We previously demonstrated that bone morphogenetic proteins (BMPs) induce cardiomyocyte differentiation through the mitogen-activated protein kinase
临床实验结果喜人！NEJM 揭示新型四价登革热疫苗有效性可达 80.2%
2019 年 11 月 6 号，世界前十药企的日本制药巨头武田药品 (Takeda) 的团队在 The New England Journal of Medicine 发表了题为《Efficacy of a Tetravalent Dengue Vaccine in Healthy Children and Adolescents》的论文，介绍了他们所研发四价登革热疫苗 TAK- 003 的大规模随机双盲临床实验结果1。该研究是针对所有四种登革热亚型设计的疫苗，TAK- 003 在随机双盲临床
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