JNJ-49095397

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

JNJ-49095397 (RV-568) 是一种特异性窄谱激酶抑制剂，可抑制一组选定的参与 COPD 炎症的激酶，对 p38α、p38γ 和 HCK 的 IC50 分别为 5、40 和 52 nM。

JNJ-49095397 (RV-568) is a specific narrow-spectrum kinase inhibitor that inhibits a selected set of kinases involved in COPD inflammation with IC50 of 5, 40 and 52 nM for p38α, p38γ and HCK, respectively; shows potent anti-inflammatory effects in monocytes and macrophages, demonstrates synergistic interaction in poly I:C-stimulated BEAS-2B cells and in the cigarette smoke model combined with corticosteroid.COPD Phase 2 Clinical.

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Animal Model:Nonfasted Balb/c mice, LPS-induced neutrophil accumulation model Dosage:1, 4 and 20 μg/mouse Administration:Intratracheal administration, 2, 8 or 12 h prior to LPS inhalation Result:Prevented the accumulation of neutrophils in the BAL fluid. Significantly inhibited neutrophil accumulation when administered up to 8 h prior to LPS inhalation.

RV568 | RV-568 | JNJ49095397

MAPK/ERK Signaling

p38 MAPK

p38 MAPK

Inflammation/Immunology

COPD

1220626-82-3

592.7

C34H36N6O4

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (168.72 mM)

CC1=CC=C(C=C1)N2C(=CC(=N2)C(C)(C)C)NC(=O)NC3=CC=C(C4=CC=CC=C43)OCC5=CC(=NC=C5)NC(=O)COC

N-(4-((4-(3-(3-tert-Butyl-1-p-tolyl-1H-pyrazol-5-yl)ureido)-naphthalen-1-yloxy)methyl)yridin-2-yl)-2-methoxyacetamide

(-20℃)

With Ice Pack

≥ 2 years