产品说明书

TAK-715

Print
Chemical Structure| 303162-79-0 同义名 : -
CAS号 : 303162-79-0
货号 : A302845
分子式 : C24H21N3OS
纯度 : 99%+
分子量 : 399.508
MDL号 : MFCD17012805
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(262.82 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

30% propylene glycol+5% Tween 80+65% water 30 mg/mL suspension

生物活性
靶点

  • p38β

    p38β, IC50:0.20 μM

  • p38α

    p38α, IC50:7.1 nM
描述 The stress-activated protein kinase (SAPK) p38 isoforms are mitogen-activated protein kinase (MAPK) family members. MAPKs act as an integration point for multiple biochemical signals, and are involved in a wide variety of cellular processes such as proliferation, differentiation, transcription regulation and development. The well reported isoforms of p38 MAPKs include p38α, p38β and others. TAK-715 is a p38 MAPK inhibitor, with selectivity for p38α. The inhibitory IC50 of TAK-715 against p38α was 7.1nM while the data against p38β was 200nM. TAK-715 was not active against p38γ, p38δ, or other kinases. TAK-715 inhibited LPS-stimulated release of TNFα from THP-1 cells with an IC50 of 48 nM[3]. At the concentration of 10μM, TAK-715 inhibited Wnt-3a-induced hDvl2 phosphorylation and the hDvl2 shift in U2OS-EFC cells[4]. Orally administrated at the dose of 10mg/kg, TAK-715 resulted in 87.6% inhibition of LPS-induced TNFα production in mice. In an adjuvant-induced arthritis model in rats, TAK-715 dose dependently inhibited paw swelling when given daily for 14 days at 3mg/kg, 10mg/kg or 30mg/kg[3].
作用机制 TAK-715 target p38α in an ATP-competitive manner[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.50mL

0.50mL

0.25mL

12.52mL

2.50mL

1.25mL

25.03mL

5.01mL

2.50mL
参考文献

[1]Verkaar F, van der Doelen AA, 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 Apr 22;18(4):485-94.

[2]Miwatashi S, Arikawa Y, 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 Sep 22;48(19):5966-79.

[3]Miwatashi S, Arikawa Y, Kotani E, Miyamoto M, Naruo K, Kimura H, Tanaka T, Asahi S, Ohkawa S. 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 Sep 22;48(19):5966-79.

[4]Verkaar F, van der Doelen AA, Smits JF, Blankesteijn WM, Zaman GJ. Inhibition of Wnt/β-catenin signaling by p38 MAP kinase inhibitors is explained by cross-reactivity with casein kinase Iδ/ɛ. Chem Biol. 2011 Apr 22;18(4):485-94.