1. Immunology/Inflammation Apoptosis NF-κB Metabolic Enzyme/Protease
  2. NOD-like Receptor (NLR) Pyroptosis Caspase Interleukin Related Reactive Oxygen Species (ROS)
  3. M464

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.

For research use only. We do not sell to patients.

M464

M464 Chemical Structure

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Description

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[1].

IC50 & Target[1]

NLRP3 inflammasome

 

In Vitro

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.

In Vivo

M464 (15, 30, 60 mg/kg; i.g.; single dose; 1 hour before LPS injection) mitigates LPS (HY-D1056)-induced acute lung injury in mice by inhibiting NLRP3 inflammasome activation[1].
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.
Molecular Weight

464.66

Formula

C23H28O4S3

Appearance

Solid

Color

Orange to red

SMILES

CC1CC(OC(CCC(OC2=CC=C(C3=CC(SS3)=S)C=C2)=O)=O)C(C(C)C)CC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
M464
Cat. No.:
HY-179494
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