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Chemical Structure| 6823-69-4 Chemical Structure| 6823-69-4

Structure of GW4869
CAS No.: 6823-69-4

Chemical Structure| 6823-69-4

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GW4869 2HCl is a cell permeable, selective and non-competitve inhibitor of N-SMase (neutral sphingomyelinase), which is important in the metabolism of sphingomyelin producing ceramide and phosphocholine and in cell signaling and regulation. GW4869 is an exosome inhibitor.

Synonyms: GW 4869 (hydrochloride hydrate); GW554869A; GW69A

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Product Details of GW4869

CAS No. :6823-69-4
Formula : C30H30Cl2N6O2
M.W : 577.50
SMILES Code : O=C(/C=C/C1=CC=C(C=C1)/C=C/C(NC2=CC=C(C=C2)C3=NCCN3)=O)NC4=CC=C(C=C4)C5=NCCN5.Cl.Cl
Synonyms :
GW 4869 (hydrochloride hydrate); GW554869A; GW69A
MDL No. :MFCD06411564

Safety of GW4869

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
L02 cells 20 μM 12 h To prevent exosome secretion PMC9556718
KBM7 SGMS1GT+SGMS1 cells 10 μM 24 h GW4869 treatment significantly reduced ZIKV shedding PMC7374707
Huh7 cells 10 μM 24 h GW4869 treatment reduced viral shedding PMC7374707
M2 macrophages 10 µM 8 h GW4869 successfully blocked the release of extracellular vesicles (EVs) from M2 macrophages, thereby reducing the proliferation, migration, and phenotypic transformation of CFs. PMC8120198
monocyte-derived macrophages (MDM) 2, 5, 10 μM 24 h Inhibit MV release, reduce GLS1 release PMC4635976
BV2 microglia cell line 2, 5, 10 μM 24 h Inhibit MV release, reduce GLS1 release PMC4635976
CAFs 20 μM Inhibit exosome secretion PMC8233173
cardiomyocytes 10 μM 24 h Inhibit the production of cardiomyocyte-derived EVs and reduce N1 neutrophil polarization PMC11484374
BMMs 10 μM 18 h Inhibit exosome biogenesis and prevent DNA-induced Ifnb expression PMC6433288
MEFs 10 μM 18 h Inhibit exosome biogenesis and prevent DNA-induced Ifnb expression PMC6433288
RAW264.7 cells 10 μg/mL 24 h To investigate the effect of T lymphocyte-derived EVs on macrophage migration, the results showed that EVs derived from PKM2-activated T lymphocytes significantly promoted macrophage migration. PMC8842084

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice Endometrial cancer xenograft model Intraperitoneal injection 2 mg/kg Every other day until tumor collection Inhibit CAFs-mediated tumor growth PMC8233173
mice myocardial ischemia/reperfusion injury model intraperitoneal injection 2.5 mg/kg single injection, lasting 1 hour Inhibit the production of EVs and reduce myocardial ischemia/reperfusion injury PMC11484374
mice C57BL/6N mice intraperitoneal injection 0.3125 or 1.25 µg/g once per day for five consecutive days Inhibit exosome biogenesis and reduce Ifnb mRNA and Mx1 expression, but not Tnfa mRNA PMC6433288
Mice Elastase-induced abdominal aortic aneurysm model Intraperitoneal injection 1.25 mg/kg Once daily for 21 days To investigate the effect of GW4869 on the development of abdominal aortic aneurysm, the results showed that GW4869 significantly attenuated elastase-induced AAA expansion and macrophage infiltration. PMC8842084

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.73mL

0.35mL

0.17mL

8.66mL

1.73mL

0.87mL

17.32mL

3.46mL

1.73mL

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