M464
Based on 1 Customer Validation
M464, a non-steroidal anti-inflammatory compound, is a potent and orally active NLRP3 inflammasome inhibitor. M464 inhibits pyroptosis and hinders the activation of downstream Caspase-1 expression and the release of IL-1β by impeding ASC oligomerisation and curtailing ROS production. M464 exhibits protective effects against acute lung and liver injury in mice. M464 can be used for the research of NLRP3-related inflammatory diseases.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.58%
- Fòrmula: C23H28O4S3
- Peso molecular:464.66
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Ver todos los productos específicos de isoformas Caspase
More
Actividad biológica
|
NLRP3 inflammasome |
M464 (3-12 μM) inhibits the expression of marker proteins associated with NLRP3 inflammasome activation (IL-1β and Caspase-1), and restrains the production of intracellular ROS and the formation of ASC oligomers in J774A.1 and THP-1 cells[1].
M464 (3-12 μM; 1 h) inhibits pyroptosis in macrophages triggered by the NLRP3 inflammasome stimulator in J774A.1 and THP-1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
M464 (15, 30, 60 mg/kg; i.g.; single dose; 1 hour before LPS injection) mitigates LPS and D-GalN-induced acute liver injury in mice by inhibiting NLRP3 inflammasome activation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male KM mice (42-56 days old) intraperitoneally injected with LPS (10 mg/kg)[1]
-
Dosage:15, 30, 60 mg/kg
-
Administration:i.g.; single dose; 1 hour before LPS injection
-
Result:Dose-dependently reduced the pathological scores of lung injury.
Significantly improved the lung tissue damage in mice.
Inhibited the lung wet/dry (W/D) weight ratio and significantly improved pulmonary edema in mice.
Significantly reduced the levels of mature IL-1β and Caspase-1.
-
Animal Model:Male KM mice (42-56 days old) intraperitoneally injected with LPS (50 μg/kg) and D-GalN (800 mg/kg)[1]
-
Dosage:15, 30, 60 mg/kg
-
Administration:i.g.; 1 hour before LPS injection
-
Result:Reversed the LPS and D-GalN induced increase of the liver-to-body weight ratio.
Markedly attenuated LPS/D-GalN-induced liver injury in mice.
Exhibited dose-dependent suppression of serum levels of AST and ALT.
Effectively suppressed the mature IL-1β release and Caspase-1 production in a dose-dependent manner.
Effectively reversed the LPS/D-GalN-induced reduction in SOD content and increase in MDA level.
Chemical Information
-
Appearance Solid
-
Peso molecular 464.66
-
Fòrmula C23H28O4S3
-
Color Orange to red
-
SMILES
CC1CC(OC(CCC(OC2=CC=C(C3=CC(SS3)=S)C=C2)=O)=O)C(C(C)C)CC1
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Pureza y Documentación
-
Ficha de datos (272 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)