YQ128 是选择性NLRP3 炎性体抑制剂(IC50:0.30 μM)。它能显著的、选择性抑制IL-1β的产生，但不影响 TNF-α 的产生。它能够透过血脑屏障到达中枢神经系统。它具有抗炎作用。

YQ128 is a potent and selective inhibitor of second-generation NLRP3 (NOD-like receptor P3) inflammasome(IC50 of 0.30 μM), with anti-inflammatory activity.

The release of IL-1β from peritoneal macrophages upon LPS/ATP challenge(IC50 of 1.59 μM) dose dependently suppressed by YQ128 (0.3-100 μM; 30 mins).

YQ128 (oral; 20 mg/kg) shows delayed gastrointestinal absorption with a tmax and cmax of 12 h and 73 ng/mL, respectively. YQ128 exhibits extensive extravascular distribution with a large steady-state volume of distribution (Vdss) of 8.5 L/kg and rapid total clearance (CLtot) of 41 mL/min/kg. In C57BL/6 mice, YQ128 (10 mg/kg) has been shown to trigger IL-1β production in a NLRP3- dependent manner .

2454246-18-3

C27H29ClN2O4S2

545.11

DMSO:248 mg/mL (454.95 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years