TAK-715( TAK 715 | TAK715 )

Catalog No. M13955 CAS No. 303162-79-0

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

TAK-715
Note

Research use only, not for human use.
Brief Description

A potent, selective, orally active p38α MAPK inhibitor with IC50 of 7.1 nM.
Description

A potent, selective, orally active p38α MAPK inhibitor with IC50 of 7.1 nM; displays >20-fold selectvity over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1; inhibits LPS-stimulated release of TNF-alpha from THP-1 with IC50 of 48 nM; exerts significant efficacy in rat adjuvant-induced arthritis model.Rheumatoid Arthritis Phase 2 Discontinued.
In Vitro

——
In Vivo

Animal Model:7-week-old male Lewis rats with arthritis Dosage:3, 10, 30 mg/kg Administration:PO; single dose Result:Significantly reduced the secondary paw volume (25% inhibition).Animal Model:Rat Dosage:10 mg/kg (Pharmacokinetic Analysis)Administration:PO Result:Had a Cmax of 0.19 μg/mL and an AUC of 1.16 μg?h/mL.
Synonyms

TAK 715 | TAK715
Pathway

MAPK/ERK Signaling
Target

p38 MAPK
Recptor

JNK1| p38α| p38β| p38γ| p38δ
Research Area

Inflammation/Immunology
Indication

Rheumatoid Arthritis

CAS Number

303162-79-0
Formula Weight

399.508
Molecular Formula

C24H21N3OS
Purity

>98% (HPLC)
Solubility

10 mM in DMSO
SMILES

O=C(NC1=NC=CC(C2=C(C3=CC=CC(C)=C3)N=C(CC)S2)=C1)C4=CC=CC=C4
Chemical Name

Benzamide, N-[4-[2-ethyl-4-(3-methylphenyl)-5-thiazolyl]-2-pyridinyl]-

1. Miwatashi S, et al. J Med Chem. 2005 Sep 22;48(19):5966-79. 2. Verkaar F, et al. Chem Biol. 2011 Apr 22;18(4):485-94.

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