| Hazard Information | Back Directory | [Uses]
NLRP3-IN-20 (compound 11) is an orally available inhibitor of the NLRP3 inflammasome with an IC50 of 25 nM for IL-1β secretion. NLRP3-IN-20 has excellent pharmacokinetic properties and demonstrated significant efficacy in models of non-alcoholic steatohepatitis, fatal septic shock, and colitis[1]. | [in vivo]
Pharmacokinetic Analysis in Mouse[1]
| Route | Dose (mg/kg) | T1/2 (h) | Tmax (h) | Cmax (ng/mL) | AUC0-inf (ng·h/mL) | MRT0-inf (h) | Vz (mL/kg) | Cl (mL/h/kg) | F (%) | | i.v. | 5 | 4.01 | 0.083 | 22567 | 130240/ | 5.30 | 226 | 38.8 | | | p.o. | 10 | 3.50 | 0.667 | 33867 | 221955 | 4.79 | / | / | 85.21 |
| [References]
[1] Li Z, et al. Novel Sulfonylurea-Based NLRP3 Inflammasome Inhibitor for Efficient Treatment of Nonalcoholic Steatohepatitis, Endotoxic Shock, and Colitis. J Med Chem. 2023 Sep 11.. . DOI:10.1021/acs.jmedchem.3c00894 |
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