303162-79-0|TAK-715|CsnPharm

CAS No.: 303162-79-0

TAK-715 Catalog No. CSN15958

Synonyms: TA 715

TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, being 28-fold selective for p38α over p38β, showing no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1.

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400-920-2911

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tech@csnpharm.cn

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实验方案

技术信息

生物活性

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].
临床研究
NCT号适应症或疾病临床期招募状态预计完成时间地点
NCT00760864 Arthritis, Rheumatoid Phase 2 Completed - -
参考文献

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00760864	Arthritis, Rheumatoid	Phase 2	Completed	-	-

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5031 mL
- 12.5154 mL
- 25.0308 mL
- 5 mM
- 0.5006 mL
- 2.5031 mL
- 5.0062 mL
- 10 mM
- 0.2503 mL
- 1.2515 mL
- 2.5031 mL

技术信息

CAS号

303162-79-0

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H21N3OS

运输

蓝冰

分子量

399.51

别名

TA 715

溶解度

DMSO	80.0 mg/mL (200.2 mM)
Water	Insoluble
Ethanol	16.0 mg/mL (40.0 mM)

动物实验配方

30% propylene glycol+5% Tween 80+65% water

30 mg/mL

suspension

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