TAK-715 ( TAK 715 | TAK715 )

产品货号. M13955 CAS No. 303162-79-0

COA

Datasheet

HNMR

HPLC

MSDS

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产品名称

TAK-715
注意事项

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
产品简述

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

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.
体外实验

——
体内实验

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.
同义词

TAK 715 | TAK715
通路

MAPK/ERK Signaling
靶点

p38 MAPK
受体

JNK1| p38α| p38β| p38γ| p38δ
研究领域

Inflammation/Immunology
适应症

Rheumatoid Arthritis

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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