YQ128_product_DataBase

Bioactivity

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].

Invitro

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[1]. YQ128 (20 µM; 2 hours) shows no significant toxic effects on hCMEC/D3 cells[1]. Cell Viability Assay[1] Cell Line:

In Vivo

YQ128 (iv; 20 mg/kg) has an intermediate terminal plasma half-life (t1/2) of 6.6 hours after iv administration[1]. YQ128 (oral; 20 mg/kg) shows delayed gastrointestinal absorption with a tmax and cmax of 12 h and 73 ng/mL, respectively. Oral bioavailability (Foral) is estimated as 10%[1]. 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[1]. YQ128 (10 mg/kg) has been shown to trigger IL-1β production in a NLRP3- dependent manner in C57BL/6 mice[1]. Animal Model:

Name

YQ128

CAS

2454246-18-3

Formula

C27H29ClN2O4S2

Molar Mass

545.11

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

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

PeptideDB

YQ128

CAS: 2454246-18-3 F: C27H29ClN2O4S2 W: 545.11