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GW4869

  Cat. No.:  DC7662   Featured
Chemical Structure
6823-69-4
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More than 5000 active chemicals with high quality for research!
Field of application
GW4869 is a cell permeable, selective inhibitor of N-SMase (neutral sphingomyelinase).
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 6823-69-4
Chemical Name: 2-Propenamide,3,3'-(1,4-phenylene)bis[N-[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-,dihydrochloride
Synonyms: 2-Propenamide,3,3'-(1,4-phenylene)bis[N-[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-,dihydrochloride;2-Propenamide,3,3'-(1,4-phenylene)bis[N-[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-,dihydrochlor...;GW 4869;GW 4869 (hydrochloride hydrate);GW-4869;Hydrochloride Hydrate;N,N′-Bis[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-3,3′-p-phenylene-bis-acrylamide dihydrochloride;4',4''-Di-2-imidazolin-2-yl-p-benzenediacrylanilide dihydrochloride;GW4869
SMILES: O=C(NC1=CC=C(C2=NCCN2)C=C1)/C=C/C3=CC=C(/C=C/C(NC4=CC=C(C5=NCCN5)C=C4)=O)C=C3.[H]Cl.[H]Cl
Formula: C30H28N6O2.2[HCl].H2O
M.Wt: 595.51948
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: GW4869 is a noncompetitive neutral sphingomyelinase inhibitor with an IC50 of 1 μM.
In Vivo: Pre-treatment with GW4869 significantly impairs release of both exosomes and pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) in RAW264.7 macrophages. At 12 h after LPS treatment or CLP surgery, WT mice pretreated with GW4869 displays lower amounts of exosomes and pro-inflammatory cytokines in the serum than control PBS-injected mice. Accordingly, GW4869 treatment diminishes the sepsis-induced cardiac inflammation, attenuates myocardial depression and prolongs survival[2].
In Vitro: GW4869 (10 μM) partially inhibits TNF-induced sphingomyelin (SM) hydrolysis, and 20 μM of the compound is protected completely from the loss of SM. The addition of 10-20 μM GW4869 completely inhibits the initial accumulation of ceramide, whereas this effect is partially lost at later time points (24 h). The action of GW4869 occurs downstream of the drop in glutathione. GW4869 is able, in a dose-dependent manner, to significantly protect from cell death. These protective effects are accompanied by significant inhibition of cytochrome c release from mitochondria and caspase 9 activation, therefore localizing N-SMase activation upstream of mitochondrial dysfunction[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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