YQ128 是有效的，选择性第二代 NLRP3 炎性体抑制剂，IC₅₀ 为 0.30 µM。YQ128 能显着和选择性地抑制 IL-1β 的产生，但不抑制 TNF-α 的产生。YQ128 可以穿过血脑屏障到达中枢神经系统。YQ128 具有抗炎活性。

YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC 50 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.

Solid

NLRP3 0.30 μM (IC50) IL-1β

YQ128 (0.3-100 μM; 30 mins) dose dependently suppressed the release of IL-1β from peritoneal macrophages upon LPS/ATP challenge with an IC50 of 1.59 μM.
YQ128 (20 μM; 2 hours) shows no significant toxic effects on hCMEC/D3 cells.
has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay

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 a t max and c max of 12 h and 73 ng/mL, respectively. Oral bioavailability (F oral ) 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.
YQ128 (10 mg/kg) has been shown to trigger IL-1β production in a NLRP3- dependent manner in C57BL/6 mice. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Jiang Y, et al. Discovery of Second-Generation NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization. J Med Chem. 2019 Oct 31.

In Vitro: DMSO : 250 mg/mL (458.62 mM; Need ultrasonic)配制储备液