Acumapimod

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

一种口服有效的 p38 MAPK 抑制剂，可有效抑制离体 LPS 诱导的 TNFα 分泌，IC50 为 44 ng/mL (115 nM)。

An orally active, potent p38 MAPK inhibitor that potently inhibits ex vivo LPS‐induced TNFα secretion with an IC50 of 44 ng/mL (115 nM); inhibits LPS‐stimulated TNFα release in the human whole blood assay with IC50 of 24 nM; shows antiinflammatory activity for treatment of acute as opposed to chronic inflammation disorders.COPD Phase 1 Clinical.

Acumapimod is an inhibitor of p38α with an IC50 value of less than 1 μM.

Acumapimod is an oral low-molecular-weight p38 inhibitor currently in development for the treatment of several inflammatory conditions, including chronic obstructive pulmonary disease (COPD). Intermittent short-term dosing of Acumapimod (75 mg on days 1 and 6) shows a marked improvement in lung function in COPD patients.

BCT-197

MAPK/ERK Signaling

p38 MAPK

p38 MAPK

Inflammation/Immunology

COPD

836683-15-9

385.4185

C22H19N5O2

>98% (HPLC)

DMSO: 10 mM

O=C(NC1CC1)C2=CC=C(C)C(N3N=CC(C(C4=CC=CC(C#N)=C4)=O)=C3N)=C2

Benzamide, 3-[5-amino-4-(3-cyanobenzoyl)-1H-pyrazol-1-yl]-N-cyclopropyl-4-methyl-

(-20℃)

With Ice Pack

≥ 2 years