NP3-146

NP3-146
Identifiers
	IUPAC name 1-[4-chloro-2,6-di(propan-2-yl)phenyl]-3-[4-(2-hydroxypropan-2-yl)furan-2-yl]sulfonylurea;
CAS Number	210826-47-4;
PubChem CID	10195003;
ChemSpider	8370503;
ChEMBL	ChEMBL5397828;
Chemical and physical data
Formula	C20H27ClN2O5S
Molar mass	442.96 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC(C)C1=CC(=CC(=C1NC(=O)NS(=O)(=O)C2=CC(=CO2)C(C)(C)O)C(C)C)Cl;
	InChI InChI=1S/C20H27ClN2O5S/c1-11(2)15-8-14(21)9-16(12(3)4)18(15)22-19(24)23-29(26,27)17-7-13(10-28-17)20(5,6)25/h7-12,25H,1-6H3,(H2,22,23,24); Key:RTJGVFANTDWUEG-UHFFFAOYSA-N;

NP3-146 (NLRP3-IN-5) is an experimental drug which acts as an inhibitor of the NLRP3 inflammasome. It inhibits the release of interleukin-1β and interleukin-18 which is usually triggered by inflammatory stimuli, and so terminates the resulting signalling cascade. It is used for research into various conditions in which chronic inflammation plays a role.^[1]^[2]^[3]^[4]

References

↑ Dekker C, Mattes H, Wright M, Boettcher A, Hinniger A, Hughes N, et al. (December 2021). "Crystal Structure of NLRP3 NACHT Domain With an Inhibitor Defines Mechanism of Inflammasome Inhibition". Journal of Molecular Biology. 433 (24) 167309. doi:10.1016/j.jmb.2021.167309. PMID 34687713.
↑ Gastaldi S, Rocca C, Gianquinto E, Granieri MC, Boscaro V, Blua F, et al. (September 2023). "Discovery of a novel 1,3,4-oxadiazol-2-one-based NLRP3 inhibitor as a pharmacological agent to mitigate cardiac and metabolic complications in an experimental model of diet-induced metaflammation". European Journal of Medicinal Chemistry. 257 115542. arXiv:2309.07939. doi:10.1016/j.ejmech.2023.115542. PMID 37290185.
↑ Ma Q (May 2023). "Pharmacological Inhibition of the NLRP3 Inflammasome: Structure, Molecular Activation, and Inhibitor-NLRP3 Interaction". Pharmacological Reviews. 75 (3): 487–520. doi:10.1124/pharmrev.122.000629. PMC 10121800. PMID 36669831.
↑ Feng H, Li D, Zhu F, Jiang C, Su M, Kong Y, et al. (December 2024). "Design, synthesis and biological evaluation of sulfonylurea derivatives as NLRP3 inflammasome inhibitors". Bioorganic & Medicinal Chemistry Letters. 114 129987. doi:10.1016/j.bmcl.2024.129987. PMID 39395633.

[1] Dekker C, Mattes H, Wright M, Boettcher A, Hinniger A, Hughes N, et al. (December 2021). "Crystal Structure of NLRP3 NACHT Domain With an Inhibitor Defines Mechanism of Inflammasome Inhibition". Journal of Molecular Biology. 433 (24) 167309. doi:10.1016/j.jmb.2021.167309. PMID 34687713.

[2] Gastaldi S, Rocca C, Gianquinto E, Granieri MC, Boscaro V, Blua F, et al. (September 2023). "Discovery of a novel 1,3,4-oxadiazol-2-one-based NLRP3 inhibitor as a pharmacological agent to mitigate cardiac and metabolic complications in an experimental model of diet-induced metaflammation". European Journal of Medicinal Chemistry. 257 115542. arXiv:2309.07939. doi:10.1016/j.ejmech.2023.115542. PMID 37290185.

[3] Ma Q (May 2023). "Pharmacological Inhibition of the NLRP3 Inflammasome: Structure, Molecular Activation, and Inhibitor-NLRP3 Interaction". Pharmacological Reviews. 75 (3): 487–520. doi:10.1124/pharmrev.122.000629. PMC 10121800. PMID 36669831.

[4] Feng H, Li D, Zhu F, Jiang C, Su M, Kong Y, et al. (December 2024). "Design, synthesis and biological evaluation of sulfonylurea derivatives as NLRP3 inflammasome inhibitors". Bioorganic & Medicinal Chemistry Letters. 114 129987. doi:10.1016/j.bmcl.2024.129987. PMID 39395633.

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See also

References