NLRP3 is an intracellular sensor that can detect various microbial motifs, endogenous danger signals, and environmental stimuli. This leads to the formation and activation of NLRP3 inflammasomes. Meanwhile, the assembly of NLRP3 inflammasomes leads to the release of caspase 1 dependent pro-inflammatory cytokines IL-1 β and IL-18, as well as gasdermin D-mediated pyroptosis cell death. Nonetheless, the abnormal activation of NLRP3 inflammasomes is associated with various inflammatory diseases. It includes cold and hot protein related periodic syndrome, Alzheimer’s disease, diabetes and atherosclerosis. Importantly, the pyridine domain of NLRP3 interacts with the pyridine domain of ASC to initiate inflammasome assembly. Particularly, the NLRP3 inflammasome is crucial for the host’s immune defense against bacterial, fungal, and viral infections. Today, we will introduce an orally active and selective NLRP3 inflammasome inhibitor for various inflammatory diseases research, Dapansutrile.

Dapansutrile is an Orally Active NLRP3 Inhibitor for Various Inflammatory Diseases Research.

Above all, Dapansutrile is a potent, orally active and selective NLRP3 inflammasome inhibitor. Additionally, Dapansutrile has anti-inflammatory activity and decreases immune factor levels. Dapansutrile can be used for research of inflammatory diseases.

Next in importance, Dapansutrile ameliorates neurological decline and nervous tissue damage in experimental autoimmune encephalomyelitis (EAE) mice. Interestingly, Dapansutrile attenuates the protein levels of pro-inflammatory cytokines in the spinal cord of EAE mice.
Once again, Dapansutrile reduces infarct size and reduces caspase-1 activity in the heart in male ICR (CD1) mice. Obviously, Dapansutrile preserves cardiac function following myocardial ischemia-reperfusion injury.

All in all, Dapansutrile is an orally active and selective NLRP3 inflammasome inhibitor for various inflammatory diseases research.


Sánchez-Fernández A, et, al. Front Immunol. 2019 Nov 1;10:2578.