YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC50 of 0.30 μM. YQ128 significantly and selectively suppresses the production of IL-1β, but not TNF-α, and it can cross the BBB to reach the CNS. YQ128 has anti-inflammatory activity[1]. YQ128 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
YQ128 is a potent and selective second-generation NLRP3 inflammasome inhibitor with IC50 of 0.30 μM. YQ128 significantly and selectively inhibited the production of IL-1β, but not TNF-α. YQ128 can cross the blood-brain barrier to reach the central nervous system. YQ128 has anti-inflammatory activity.
YQ128 (0.3-100 μM; 30 mins) dose dependently suppressed the release of IL-1β from peritoneal macrophages upon LPS/ATP challenge with an IC 50 of 1.59 μM.
YQ128 (20 μM; 2 hours) shows no significant toxic effects on hCMEC/D3 cells.
Cell Viability Assay
< td class="col1"> Cell Line: | Mouse peritoneal macrophages |
| Concentration: | 0.3, 1.0, 3.0, 10, 30, 100 μM |
| Incubation Time: | 30 mins |
| Result: | Suppressed the release of IL-1β from peritoneal macrophages upon LPS/ATP challenge with an IC 50 of 1.59 μM. |
YQ128 (iv; 20 mg/kg) has an intermediate terminal plasma half-life (t 1/2 ) of 6.6 hours after iv administration.
YQ128 (oral ; 20 mg/kg) shows delayed gastrointestinal absorption with at max and c max of 12 h and 73 ng/mL, respectively. Oral bioavailability (F oral < /sub> ) is estimated as 10%.
YQ128 exhibits extensive extravascular distribution with a large steady-state volume of distribution (Vd ss ) of 8.5 L/kg and rapid total clearance (CL tot ) of 41 mL/min/kg.
has been shown to trigger IL-1β production in a NLRP3-dependent manner in C57BL/6 mice. < /p>
< tr> | Animal Model: | Sprague-Dawley rats (200-250 g) | | Dosage: | 20 mg/kg (Pharmacokinetic Analysis) |
Administration: | Iv |
| Result: | < td class="col2"> Had an intermediate terminal plasma half-life (t 1/2 ) of 6.6 hours after iv administration.
NLRP3: 0.30 μM (IC50); IL-1β
