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產品描述： 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 |
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靶點：
p38α：7.1 nM (IC50)；p38β：200 nM (IC50)；p38δ：>10 μM (IC50)；p38γ：>10 μM (IC50)；CK1δ；CK1ε ;p38MAPK;CaseinKinase;JNK |
體內研究：
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. |
參考文獻：
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/?. 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. |
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溶解性：
DMSO : ≥ 100 mg/mL (250.31 mM) |
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保存條件：
-20℃ |
配置溶液濃度參考：
|
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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| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
北京