TAK-715

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WARNING: This product is for research use only, not for human or veterinary use.

Description:TAK-715 is a potent p38 MAPK inhibitor. which displays potent inhibitory activity (inhibition of p38alpha, IC50 = 7.1 nM; LPS-stimulated release of TNF-alpha from THP-1, IC50 = 48 nM; LPS-induced TNF-alpha production in mice, 87.6% inhibition at 10 mg/kg, po) and no inhibitory activity for major CYPs, including CYP3A4. TAK-715 was selected as a clinical candidate and is now under clinical investigation for the treatment of RA.

Price and Availability

TAK-715, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide).

Synonym:TAK715, TA 715, TAK715

IUPAC/Chemical Name:N-(4-(2-ethyl-4-(m-tolyl)thiazol-5-yl)pyridin-2-yl)benzamide

InChi Key:HEKAIDKUDLCBRU-UHFFFAOYSA-N

InChi Code:InChI=1S/C24H21N3OS/c1-3-21-27-22(18-11-7-8-16(2)14-18)23(29-21)19-12-13-25-20(15-19)26-24(28)17-9-5-4-6-10-17/h4-15H,3H2,1-2H3,(H,25,26,28)

SMILES Code:O=C(NC1=NC=CC(C2=C(C3=CC=CC(C)=C3)N=C(CC)S2)=C1)C4=CC=CC=C4

Technical Data

References

1: Falck D, Kool J, Honing M, Niessen WM. Tandem massspectrometry study of p38α kinase inhibitors and related substances. JMass Spectrom. 2013 Jun;48(6):718-31. doi: 10.1002/jms.3219. PubMedPMID: 23722963.

2: Azevedo R, van Zeeland M, Raaijmakers H, Kazemier B, de Vlieg J,Oubrie A. X-ray structure of p38α bound to TAK-715: comparison withthree classic inhibitors. Acta Crystallogr D Biol Crystallogr. 2012Aug;68(Pt 8):1041-50. doi: 10.1107/S090744491201997X. Epub 2012 Jul 17.PubMed PMID: 22868770.

3: Verkaar F, van der Doelen AA, Smits JF, Blankesteijn WM, Zaman GJ.Inhibition of Wnt/β-catenin signaling by p38 MAP kinase inhibitors isexplained by cross-reactivity with casein kinase Iδ/ɛ. Chem Biol. 2011Apr 22;18(4):485-94. doi: 10.1016/j.chembiol.2011.01.015. PubMed PMID:21513885.

4: 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 ananti-TNF-alpha drug: discovery ofN-[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. PubMed PMID: 16162000.

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