TAK-715

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、口服活性的 p38α MAPK 抑制剂，IC50 为 7.1 nM。

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.

——

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.

TAK 715 | TAK715

MAPK/ERK Signaling

p38 MAPK

JNK1| p38α| p38β| p38γ| p38δ

Inflammation/Immunology

Rheumatoid Arthritis

303162-79-0

399.508

C24H21N3OS

>98% (HPLC)

10 mM in DMSO

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

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

(-20℃)

With Ice Pack

≥ 2 years