Tak-715

Tak-715 Basic information
Product Name:Tak-715
Synonyms:Tak-715;N-(4-(2-Ethyl-4-(3-methylphenyl)-thiazol-5-yl)pyridin-2-yl)benzamide;BenzaMide, N-[4-[2-ethyl-4-(3-Methylphenyl)-5-thiazolyl]-2-pyridinyl]-;N-(4-(2-Ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl)-2-pyridyl)benzamide;N-(4-(2-Ethyl-4-(m-tolyl)thiazol-5-yl)pyridin-2-yl)benzamide;N-[4-[2-Ethyl-4-(3-methylphenyl)-5-thiazolyl]-2-pyridinyl]benzamide;TAK-715; TAK715;CS-1566
CAS:303162-79-0
MF:C24H21N3OS
MW:399.51
EINECS:
Product Categories:Inhibitors;MAPK
Mol File:303162-79-0.mol
Tak-715 Structure
Tak-715 Chemical Properties
storage temp. Sealed in dry,2-8°C
solubility DMSO: >15mg/mL
form powder
color faint yellow to dark yellow
Safety Information
Hazard Codes Xn
Risk Statements 22-36
Safety Statements 26
WGK Germany 3
HS Code 2934999090
MSDS Information
Tak-715 Usage And Synthesis
UsesTAK 715 is a p38 MAPK inhibitor for p38α and p38β but not for p38γ and p38δ.
DefinitionChEBI: N-[4-[2-ethyl-4-(3-methylphenyl)-5-thiazolyl]-2-pyridinyl]benzamide is a member of benzamides.
Biological Activitytak-715 is a selective inhibitor of p38 mapk with ic50 value of 7.1 nm [1].p38 mitogen-activated protein (map) kinases (p38 mapks) are a class of mitogen-activated protein kinases and play an important role in controlling cellular responses to cytokines and stress. four p38 mapks contain members, p38-α (mapk14), p38-β (mapk11), p38-γ (mapk12/erk6), and p38-δ (mapk13/sapk4), have been identified. abnormal expression of p38 mapks are correlated with a variety of chronic inflammatory diseases and their inhibitors are regarded as promising targets in clinical [1] [2].tak-715 is a potent p38 mapk inhibitor and has a different selectivity with the reported p38 mapk inhibitor vx-745. when tested with human monocytic thp-1 cells, administration of tak-715 exhibited inhibition on p38mapkα with ic50 value of 7.1 nm [1]. in hek293t, u2os, and f9 cells, tak-715 was used to inhibit p38 mapk activity and concluded that p38 mapk had no function in wnt/β-catenin signaling pathway [2].in adjuvant-induced rheumatoid arthritis rat model, administration of tak-715 at dose of 10 mg/kg significantly decreased lps-induced stimulated release of tnf-α (87.6%) by inhibiting p38 mapk activity [1].
storage+4°C
references[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): p. 5966-79.
[2]. verkaar, f., et al., inhibition of wnt/beta-catenin signaling by p38 map kinase inhibitors is explained by cross-reactivity with casein kinase idelta/varepsilon. chem biol, 2011. 18(4): p. 485-94.
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