JNJ-49095397( RV568 | RV-568 | JNJ49095397 )

Catalog No. M10833 CAS No. 1220626-82-3

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Product Name

JNJ-49095397
Note

Research use only, not for human use.
Brief Description

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.
Description

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.
In Vitro

——
In Vivo

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.
Synonyms

RV568 | RV-568 | JNJ49095397
Pathway

MAPK/ERK Signaling
Target

p38 MAPK
Recptor

p38 MAPK
Research Area

Inflammation/Immunology
Indication

COPD

CAS Number

1220626-82-3
Formula Weight

592.7
Molecular Formula

C34H36N6O4
Purity

>98% (HPLC)
Solubility

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

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
Chemical Name

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

1. Onions ST, et al. J Med Chem. 2016 Mar 10;59(5):1727-46. 2. Charron CE, et al. Eur Respir J. 2017 Oct 26;50(4). pii: 1700188.

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